thiourea

Summary

Summary: A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.

Top Publications

  1. ncbi A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stress
    Michael Boyce
    Department of Cell Biology, Harvard Medical School, Boston, MA 02115, USA
    Science 307:935-9. 2005
  2. ncbi Synthesis, spectroscopic properties and antipathogenic activity of new thiourea derivatives
    Carmen Limban
    Pharmaceutical Chemistry Department, University of Medicine and Pharmacy Carol Davila, Bucharest, Romania
    Molecules 16:7593-607. 2011
  3. ncbi Autophagy regulates endoplasmic reticulum stress in ischemic preconditioning
    Rui Sheng
    Department of Pharmacology and Laboratory of Aging and Nervous Diseases, Soochow University School of Medicine, Suzhou, China
    Autophagy 8:310-25. 2012
  4. ncbi Endoplasmic reticulum stress-mediated apoptosis of EBV-transformed B cells by cross-linking of CD70 is dependent upon generation of reactive oxygen species and activation of p38 MAPK and JNK pathway
    Ga Bin Park
    Department of Anatomy and Research Center for Tumor Immunology, Inje University College of Medicine, Busan, Korea
    J Immunol 185:7274-84. 2010
  5. pmc Improved ligand-protein binding affinity predictions using multiple binding modes
    Eva Stjernschantz
    Leiden Amsterdam Center for Drug Research, Division of Molecular Toxicology, Vrije Universiteit, Amsterdam, The Netherlands
    Biophys J 98:2682-91. 2010
  6. pmc SPA0355, a thiourea analogue, inhibits inflammatory responses and joint destruction in fibroblast-like synoviocytes and mice with collagen-induced arthritis
    Y R Lee
    Department of Biochemistry, Research Institute for Endocrine Sciences, and Diabetes Research Center, Chonbuk National University Medical School, Jeonju, Jeonbuk, Korea
    Br J Pharmacol 164:794-806. 2011
  7. ncbi Selective inhibition of eukaryotic translation initiation factor 2 alpha dephosphorylation potentiates fatty acid-induced endoplasmic reticulum stress and causes pancreatic beta-cell dysfunction and apoptosis
    Miriam Cnop
    Laboratory of Experimental Medicine, Universite Libre de Bruxelles, 1070 Brussels, Belgium
    J Biol Chem 282:3989-97. 2007
  8. pmc (Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators
    Shiv K Sharma
    Department of Pharmaceutical Sciences, Wayne State University, 259 Mack Avenue, Detroit, Michigan 48202, USA
    J Med Chem 53:5197-212. 2010
  9. pmc Deficiency of αB crystallin augments ER stress-induced apoptosis by enhancing mitochondrial dysfunction
    Guorui Dou
    Arnold and Beckman Macular Research Center, Doheny Eye Institute, 1355 San Pablo Street, Los Angeles, CA 90033, USA
    Free Radic Biol Med 53:1111-22. 2012
  10. ncbi Synthesis and antiviral activities of chiral thiourea derivatives containing an alpha-aminophosphonate moiety
    Mei Hang Chen
    Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, People s Republic of China
    J Agric Food Chem 57:1383-8. 2009

Detail Information

Publications299 found, 100 shown here

  1. ncbi A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stress
    Michael Boyce
    Department of Cell Biology, Harvard Medical School, Boston, MA 02115, USA
    Science 307:935-9. 2005
    ..More broadly, salubrinal demonstrates the feasibility of selective pharmacological targeting of cellular dephosphorylation events...
  2. ncbi Synthesis, spectroscopic properties and antipathogenic activity of new thiourea derivatives
    Carmen Limban
    Pharmaceutical Chemistry Department, University of Medicine and Pharmacy Carol Davila, Bucharest, Romania
    Molecules 16:7593-607. 2011
    ..presence of one iodine, bromide or fluorine, and two or three chloride atoms on the N-phenyl substituent of the thiourea moiety, being significant especially on Pseudomonas aeruginosa and Staphylococcus aureus strains, known for their ..
  3. ncbi Autophagy regulates endoplasmic reticulum stress in ischemic preconditioning
    Rui Sheng
    Department of Pharmacology and Laboratory of Aging and Nervous Diseases, Soochow University School of Medicine, Suzhou, China
    Autophagy 8:310-25. 2012
    ..These results demonstrated that pre-activation of autophagy by ischemic preconditioning can boost endogenous defense mechanisms to upregulate molecular chaperones, and hence reduce excessive ER stress during fatal ischemia...
  4. ncbi Endoplasmic reticulum stress-mediated apoptosis of EBV-transformed B cells by cross-linking of CD70 is dependent upon generation of reactive oxygen species and activation of p38 MAPK and JNK pathway
    Ga Bin Park
    Department of Anatomy and Research Center for Tumor Immunology, Inje University College of Medicine, Busan, Korea
    J Immunol 185:7274-84. 2010
    ..Our report reveals alternate mechanisms of direct apoptosis through CD70 signaling and provides data supporting CD70 as a viable target for an Ab-based therapy against EBV-related tumors...
  5. pmc Improved ligand-protein binding affinity predictions using multiple binding modes
    Eva Stjernschantz
    Leiden Amsterdam Center for Drug Research, Division of Molecular Toxicology, Vrije Universiteit, Amsterdam, The Netherlands
    Biophys J 98:2682-91. 2010
    ..The method was applied to a set of 12 compounds binding to cytochrome P450 2C9 and it displayed a root mean-square error of 2.9 kJ/mol...
  6. pmc SPA0355, a thiourea analogue, inhibits inflammatory responses and joint destruction in fibroblast-like synoviocytes and mice with collagen-induced arthritis
    Y R Lee
    Department of Biochemistry, Research Institute for Endocrine Sciences, and Diabetes Research Center, Chonbuk National University Medical School, Jeonju, Jeonbuk, Korea
    Br J Pharmacol 164:794-806. 2011
    ..We previously synthesized a thiourea analogue, SPA0355, which suppressed NF-κB activity...
  7. ncbi Selective inhibition of eukaryotic translation initiation factor 2 alpha dephosphorylation potentiates fatty acid-induced endoplasmic reticulum stress and causes pancreatic beta-cell dysfunction and apoptosis
    Miriam Cnop
    Laboratory of Experimental Medicine, Universite Libre de Bruxelles, 1070 Brussels, Belgium
    J Biol Chem 282:3989-97. 2007
    ..This modifies the present paradigm regarding the beneficial role of eIF2alpha phosphorylation in beta-cells and must be taken into consideration when designing therapies to protect beta-cells in type 2 diabetes...
  8. pmc (Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators
    Shiv K Sharma
    Department of Pharmaceutical Sciences, Wayne State University, 259 Mack Avenue, Detroit, Michigan 48202, USA
    J Med Chem 53:5197-212. 2010
    ..These compounds represent an important new series of epigenetic modulators with the potential for use as antitumor agents...
  9. pmc Deficiency of αB crystallin augments ER stress-induced apoptosis by enhancing mitochondrial dysfunction
    Guorui Dou
    Arnold and Beckman Macular Research Center, Doheny Eye Institute, 1355 San Pablo Street, Los Angeles, CA 90033, USA
    Free Radic Biol Med 53:1111-22. 2012
    ..Thus, these data collectively demonstrate that αB crystallin provides critical protection of mitochondrial function during ER stress-induced RPE apoptosis...
  10. ncbi Synthesis and antiviral activities of chiral thiourea derivatives containing an alpha-aminophosphonate moiety
    Mei Hang Chen
    Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, People s Republic of China
    J Agric Food Chem 57:1383-8. 2009
    ..5, 50.4, and 50.4%, respectively) as the commercial product Ningnanmycin (56.2%). This would appear to be the first report of the synthesis and antiviral activity of chiral thiourea derivatives containing an alpha-aminophosphonate moiety.
  11. pmc Attractive noncovalent interactions in asymmetric catalysis: links between enzymes and small molecule catalysts
    Robert R Knowles
    Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA
    Proc Natl Acad Sci U S A 107:20678-85. 2010
    ..This perspective will outline some recent efforts to elucidate the cooperative mechanisms responsible for stereoinduction in highly enantioselective reactions promoted by noncovalent catalysts...
  12. pmc Synergistic apoptosis induction in leukemic cells by the phosphatase inhibitor salubrinal and proteasome inhibitors
    Hannes C A Drexler
    Department of Vascular Cell Biology, Max Planck Institute for Molecular Biomedicine, Muenster, Germany
    PLoS ONE 4:e4161. 2009
    ....
  13. ncbi Superoxide, H2O2, and iron are required for TNF-alpha-induced MCP-1 gene expression in endothelial cells: role of Rac1 and NADPH oxidase
    Xi Lin Chen
    Athero Genics, Inc, 8995 Westside Parkway, Alpharetta, GA 30004, USA
    Am J Physiol Heart Circ Physiol 286:H1001-7. 2004
    ..These data suggest that ROS such as superoxide and H(2)O(2) derived from Rac1-activated NADPH oxidase mediate TNF-alpha-induced MCP-1 expression in endothelial cells...
  14. ncbi A pharmacoproteomic approach implicates eukaryotic elongation factor 2 kinase in ER stress-induced cell death
    M Boyce
    Department of Cell Biology, Harvard Medical School, Boston, MA, USA
    Cell Death Differ 15:589-99. 2008
    ..Our work identifies eEF-2K as a new component of the ER stress response and underlines the utility of novel small molecules in discovering new cell biology...
  15. pmc Effect of SEA0400, a novel inhibitor of sodium-calcium exchanger, on myocardial ionic currents
    Hikaru Tanaka
    Department of Pharmacology, Toho University School of Pharmaceutical Sciences, Funabashi, Chiba 274 8510, Japan
    Br J Pharmacol 135:1096-100. 2002
    ..These results indicate that SEA0400 is a potent and highly selective inhibitor of NCX, and would be a powerful tool for further studies on the role of NCX in the heart and the therapeutic potential of its inhibition...
  16. pmc Sex differences in the effects of inherited bitter thiourea sensitivity on body weight in 4-6-year-old children
    Kathleen L Keller
    Department of Research Medicine and the New York Obesity Research Center, St Luke s Roosevelt Hospital Center, Columbia University College of Physicians and Surgeons, New York, New York, USA
    Obesity (Silver Spring) 18:1194-200. 2010
    ..These results suggest that the TAS2R38 variation, PROP phenotype, and sex interact to impact obesity risk in children. Future studies should be done to determine how this trait influences energy balance...
  17. pmc MreB drives de novo rod morphogenesis in Caulobacter crescentus via remodeling of the cell wall
    Constantin N Takacs
    Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, Connecticut 06520, USA
    J Bacteriol 192:1671-84. 2010
    ..Our results provide insight into MreB function in peptidoglycan remodeling and rod shape morphogenesis and suggest that MreB promotes the transglycosylase activity of penicillin-binding proteins...
  18. pmc Isothioureas: potent inhibitors of nitric oxide synthases with variable isoform selectivity
    G J Southan
    William Harvey Research Institute, St Bartholomew s Hospital Medical College, London
    Br J Pharmacol 114:510-6. 1995
    ....
  19. ncbi Induction of autophagic cell death by a novel molecule is increased by hypoxia
    Marco Tafani
    Department of Cellular and Molecular Pathology, IRCCS San Raffaele Pisana, Rome, Italy
    Autophagy 4:1042-53. 2008
    ..These results indicate that activation of the autophagic pathway in hypoxic cells by the new molecule CR 3294, as well as by TFP or SW, can have potentially important implications for cancer treatment...
  20. ncbi Lewis acid properties of zinc(II) in Its cyclen complex. The structure of [Zn(cyclen)(S=C(NH2)2](ClO4)2 and the bonding of thiourea to metal ions. Some implications for zinc metalloenzymes
    Michael H Salter
    Department of Chemistry, University of North Carolina at Wilmington, North Carolina 28403, USA
    Inorg Chem 44:2791-7. 2005
    ..structure of the complex [Zn(cyclen)Tu](NO(3))(2) (1) is reported (cyclen = 1,4,7,10-tetraazacyclododecane; Tu = thiourea): orthorhombic, space group P2(1)2(1)2(1), a = 11.4170(11) A, b = 12.1995(11) A, c = 12.5299(12) A, Z = 4, R = 0...
  21. ncbi Development of chiral thiourea catalysts and its application to asymmetric catalytic reactions
    Yoshiji Takemoto
    Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida, Sakyo ku, Kyoto 606 8501, Japan
    Chem Pharm Bull (Tokyo) 58:593-601. 2010
    We have developed several multifunctional thiourea catalysts bearing a tertiary amine or an 1,2-amino alcohol in expectation of their synchronous activation of a nucleophile and an electrophile through both acid-base and hydrogen-bonding ..
  22. ncbi Na+-Ca2+ exchanger contributes to Ca2+ extrusion in ATP-stimulated endothelium of intact rat aorta
    Roberto Berra-Romani
    School of Medicine, Department of Biomedicine, 13 Sur 2702, Colonia Volcanes, 72000 Puebla, Mexico
    Biochem Biophys Res Commun 395:126-30. 2010
    ..These data show that, within the same preparation, NCX operates in both modes, depending on the chemical nature of the extracellular stimulus...
  23. ncbi Fluorescence enhancement of coumarin thiourea derivatives by Hg2+, Ag+, and silver nanoparticles
    Ahmed S Al-Kady
    Chemistry Department, Faculty of Science, Tanta University, Tanta, Egypt
    J Phys Chem A 113:9474-84. 2009
    ..was observed with Fe(3+), Co(2+), Ni(2+), Cu(2+), Zn(2+), Cd(2+), La(3+), and Ce(3+), making the present coumarin thiourea derivatives selective chemosensors of both Hg(2+) and Ag(+) ions with different complexation time scales between ..
  24. ncbi Synthesis, characterization and biological evaluation of some thiourea derivatives bearing benzothiazole moiety as potential antimicrobial and anticancer agents
    Sohail Saeed
    Department of Chemistry, Research Complex, Allama Iqbal Open University, Islamabad, Pakistan
    Eur J Med Chem 45:1323-31. 2010
    Five series of thiourea derivatives bearing benzothiazole moiety (20 compounds) were efficiently synthesized and evaluated for antimicrobial and anticancer activities...
  25. ncbi Synthesis and evaluation of a thiourea-modified chitosan derivative applied for adsorption of Hg(II) from synthetic wastewater
    Lin Wang
    Institute of Oceanology, The Chinese Academy of Sciences, Qingdao 266071, China
    Int J Biol Macromol 46:524-8. 2010
    In this work, a thiourea-modified chitosan derivative (TMCD) was synthesized through two steps, O-carboxymethylated first and then modified by a polymeric Schiff's base of thiourea/glutaraldehyde...
  26. ncbi Therapeutic potential of novel Na+-Ca2+ exchange inhibitors in attenuating ischemia-reperfusion injury
    Candace Lee
    Institute of Cardiovascular Sciences, St Boniface General Hospital Research Centre, Department of Physiology, Faculty of Medicine, University of Manitoba, Winnipeg, Canada
    Can J Cardiol 21:509-16. 2005
    ..Novel NCX inhibitors discovered in recent years have shown great promise in attenuating ischemia-reperfusion injury...
  27. ncbi Synthesis and microbiological activity of thiourea derivatives of 4-azatricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione
    Marta Struga
    Medical University, Department of Medical Chemistry, 3 Oczki Str, 02 007 Warsaw, Poland
    Arch Pharm Res 33:47-54. 2010
    A series of thiourea derivatives of 4-azatricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione were synthesized. The compounds were investigated for antibacterial activity, including Gram-positive cocci, Gram-negative rods, and antifungal activity...
  28. ncbi Antitumor activity of a new N-substituted thiourea derivative, an EGFR signaling-targeted inhibitor against a panel of human lung cancer cell lines
    Xishan Xiong
    Nephrology institute of PLA, Department of Internal Medicine, Changzheng Hospital, Second Military Medical University, Shanghai, PR China
    Chemotherapy 54:463-74. 2008
    ..design and synthesis of a novel class of PTK inhibitors featuring the N-(2-oxo-1,2-dihydro-quinolin-3-ylmethyl)-thiourea framework...
  29. ncbi Theoretical studies on the bifunctionality of chiral thiourea-based organocatalysts: competing routes to C-C bond formation
    Andrea Hamza
    Institute of Structural Chemistry, Chemical Research Center of the Hungarian Academy of Sciences, Pusztaszeri ut 59 67, H 1025 Budapest, Hungary
    J Am Chem Soc 128:13151-60. 2006
    The mechanism of enantioselective Michael addition of acetylacetone to a nitroolefin catalyzed by a thiourea-based chiral bifunctional organocatalyst is investigated using density functional theory calculations...
  30. ncbi Antinociceptive pharmacology of N-(4-chlorobenzyl)-N'-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea, a high-affinity competitive antagonist of the transient receptor potential vanilloid 1 receptor
    Lei Tang
    Department of Biopharmaceutical Sciences, and Cancer Center, University of Illinois, 833 South Woods St, Chicago, IL 60612, USA
    J Pharmacol Exp Ther 321:791-8. 2007
    ..Recently, N-(4-chlorobenzyl)-N'-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea (IBTU) was synthesized, and it was found in vitro to be a high-affinity competitive antagonist of cytoplasmic, ..
  31. ncbi Transformation of herbicide propachlor by an agrochemical thiourea
    Wei Zheng
    Department of Environmental Sciences, University of California, Riverside, California 92521, USA
    Environ Sci Technol 38:6855-60. 2004
    ..to remove propachlor residues from the environment via chemical remediation by the nitrification inhibitor thiourea. The transformation processes of propachlor and thiourea mixed in aqueous solution, sand, and soil were ..
  32. pmc The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter
    J Santo-Domingo
    Departamento de Bioquimica y Biologia Molecular y Fisiologia, Facultad de Medicina, Instituto de Biologia y Genetica Molecular, Universidad de Valladolid and Consejo Superior de Investigaciones Cientificas, Valladolid, Spain
    Br J Pharmacol 151:647-54. 2007
    The thiourea derivative KB-R7943, originally developed as inhibitor of the plasma membrane Na(+)/Ca(2+) exchanger, has been shown to protect against myocardial ischemia-reperfusion injury...
  33. ncbi Organocatalytic claisen rearrangement: theory and experiment
    Martin Kirsten
    Physical Organic Chemistry, Technical University Dresden, D 01069 Dresden, Germany
    J Org Chem 72:4001-11. 2007
    ..DFT calculations employing different basis sets were utilized to predict a catalytic cycle for the thiourea-catalyzed Claisen rearrangement...
  34. ncbi Dissolving cellulose in a NaOH/thiourea aqueous solution: a topochemical investigation
    Lifeng Yan
    Hefei National Laboratory for Physical Science at Micrometer Scale and Department of Chemical Physics, University of Science and Technology of China, Hefei 230026, China
    Macromol Biosci 7:1139-48. 2007
    ..by the deposition of the suspensions of microcrystalline cellulose in water in the presence or in absence of NaOH/thiourea at different temperatures...
  35. ncbi Synthesis of acyl thiourea derivatives of chitosan and their antimicrobial activities in vitro
    Zhimei Zhong
    Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China
    Carbohydr Res 343:566-70. 2008
    Three different acyl thiourea derivatives of chitosan (CS) were synthesized and their structures were characterized by FT-IR spectroscopy and elemental analysis...
  36. ncbi Synthesis, characterization and in vitro antibacterial activity of thiourea and urea derivatives of steroids
    Salman Ahmad Khan
    Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India
    Eur J Med Chem 43:2272-7. 2008
    Some heterocyclic systems namely stigmest-6-en-7, 5alpha thiourea and stigmest-6-en-7, 5alpha urea derivatives of steroids were synthesized by the reaction of stigmest-5-en-7 one with thiourea/urea in the presence of a few drops of conc...
  37. ncbi Fluorescent labelled thiourea-bridged glycodendrons
    Pavel Krist
    Institute of Microbiology, Academy of Sciences of the Czech Republic, Videnska 1083, 142 20 Prague 4, Czech Republic
    Chembiochem 5:445-52. 2004
    ..These studies are useful for probing the mechanism of action and fate of artificial ligands and the cell receptors involved...
  38. ncbi Asymmetric 1,4-addition of oxazolones to nitroalkenes by bifunctional cinchona alkaloid thiourea organocatalysts: synthesis of alpha,alpha-disubstituted alpha-amino acids
    José Alemán
    Danish National Research Foundation Center for Catalysis, Department of Chemistry, Aarhus University, 8000 Aarhus C, Denmark
    Chemistry 14:10958-66. 2008
    ..The addition of oxazolones to nitroalkenes catalyzed by thiourea cinchona derivatives provides the corresponding alpha,alpha-quaternary alpha-amino acid derivatives with good ..
  39. pmc Thiourea modulates the expression and activity profile of mtATPase under salinity stress in seeds of Brassica juncea
    A K Srivastava
    Nuclear Agriculture and Biotechnology Division, Bhabha Atomic Research Center, Mumbai, India
    Ann Bot 103:403-10. 2009
    ..b>Thiourea (TU) has been identified as an effective bioregulator imparting stress tolerance to crops...
  40. ncbi Synthesis and antitumor activity of optically active thiourea and their 2-aminobenzothiazole derivatives: a novel class of anticancer agents
    S N Manjula
    Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Madhav Nagar, Manipal, Karnataka, India
    Eur J Med Chem 44:2923-9. 2009
    ..MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] cytotoxicity studies the optically active thiourea derivatives (IVe, IVf and IVh) were found most effective...
  41. pmc Weak Brønsted acid-thiourea co-catalysis: enantioselective, catalytic protio-Pictet-Spengler reactions
    Rebekka S Klausen
    Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA
    Org Lett 11:887-90. 2009
    The development of one-pot imine formation and asymmetric Pictet-Spengler reactions cocatalyzed by a chiral thiourea and benzoic acid is described...
  42. ncbi Novel broad-spectrum thiourea non-nucleoside inhibitors for the prevention of mucosal HIV transmission
    OSMOND J D'CRUZ
    Drug Discovery Program, Parker Hughes Institute, St Paul, Minnesota 55113, USA
    Curr HIV Res 4:329-45. 2006
    ..This review summarizes the discovery of highly potent tight binding phenethyl-thiazolyl-thiourea (PETT) derivatives targeting the NNI binding pocket of HIV-1 RT...
  43. ncbi Synthesis and biological activity of substituted urea and thiourea derivatives containing 1,2,4-triazole moieties
    Bedia Kocyigit-Kaymakcioglu
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Haydarpasa 34668, Istanbul, Turkey
    Molecules 18:3562-76. 2013
    A series of novel thiourea and urea derivatives containing 1,2,4-triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity...
  44. ncbi Disubstituted thiourea derivatives and their activity on CNS: synthesis and biological evaluation
    Joanna Stefanska
    Department of Pharmaceutical Microbiology, Medical University, 02 007 Warsaw, Poland
    Eur J Med Chem 55:205-13. 2012
    A series of new thiourea derivatives of 1,2,4-triazole have been synthesized. The difference in structures of obtained compounds are directly connected with the kind of isothiocyanate (aryl/alkyl)...
  45. ncbi Isothiourea-catalysed asymmetric C-acylation of silyl ketene acetals
    Philip A Woods
    Department EaStCHEM, School of Chemistry, University of St Andrews, North Haugh, St Andrews, Fife, KY16 9ST, UK
    Chemistry 17:11060-7. 2011
    ..Under optimised conditions 3-acyl-3-aryl or 3-acyl-3-alkylfuranones are prepared in good yields and moderate to excellent enantioselectivities (up to 98% ee; ee=enantiomeric excess)...
  46. ncbi Synthesis and bioactivity of pyrazole acyl thiourea derivatives
    Jian Wu
    State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, China
    Molecules 17:5139-50. 2012
    Sixteen novel pyrazole acyl thiourea derivatives 6 were synthesized from monomethylhydrazine (phenylhydrazine) and ethyl acetoacetate...
  47. ncbi Thiourea orchestrates regulation of redox state and antioxidant responses to reduce the NaCl-induced oxidative damage in Indian mustard (Brassica juncea (L.) Czern.)
    Ashish K Srivastava
    Nuclear Agriculture and Biotechnology Division, Bhabha Atomic Research Centre, Mumbai 400085, India
    Plant Physiol Biochem 49:676-86. 2011
    b>Thiourea (TU) has been found to enhance the stress tolerance of plants in our earlier field trials...
  48. ncbi A novel pyrimidine derivatives with aryl urea, thiourea and sulfonamide moieties: synthesis, anti-inflammatory and antimicrobial evaluation
    Ashish P Keche
    Department of Chemistry, Maharashtra Udaygiri Mahavidayla, Udgir, India
    Bioorg Med Chem Lett 22:3445-8. 2012
    ..The compounds 10, 12, 13, 18, 20, 22, 24 and 25 found to have promising antimicrobial activity against all the selected pathogenic bacteria and fungi...
  49. ncbi Selective inclusion of PO4(3-) within persistent dimeric capsules of a tris(thiourea) receptor and evidence of cation/solvent sealed unimolecular capsules
    Sandeep Kumar Dey
    Department of Chemistry, Indian Institute of Technology Guwahati, Assam 781 03, India
    Dalton Trans 41:8960-72. 2012
    A tren-based tris(thiourea) receptor, L with electron-withdrawing p-nitrophenyl terminals has been established as a competent hydrogen-bonding scaffold that can selectively encapsulate PO(4)(3-) within persistent and rigid dimeric ..
  50. ncbi Design and synthesis of thiourea derivatives containing a benzo[5,6]cyclohepta[1,2-b]pyridine moiety as potential antitumor and anti-inflammatory agents
    Wukun Liu
    Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, Nanjing, PR China
    Bioorg Med Chem Lett 22:2701-4. 2012
    b>Thiourea derivatives (6a-e) were developed and screened for antitumor and anti-inflammatory activity...
  51. ncbi N-(3-Acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea derivatives as potent vanilloid receptor agonists and analgesics
    J Lee
    Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, South Korea
    Bioorg Med Chem 9:19-32. 2001
    A series of N-(3-acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea derivatives were investigated as vanilloid receptor ligands in an effort to discover a novel class of analgesics...
  52. ncbi Thiourea compound AW00178 sensitizes human H1299 lung carcinoma cells to TRAIL-mediated apoptosis
    Byung Jun Ryu
    Laboratory of Chemical Genomics, Pharmacology Research Center, Korea Research Institute of Chemical Technology, PO Box 107, Yuseong Gu, Daejeon 305 600, Republic of Korea
    Bioorg Med Chem Lett 22:3862-5. 2012
    ..In this study, we found that 1-(5-chloro-2-methyl-phenyl)-3-[4-(5-trifluoromethyl-pyrazol-1-yl)-phenyl]-thiourea (AW00178) was able to sensitize TRAIL-resistant human lung cancer H1299 cells to TRAIL-mediated apoptosis...
  53. ncbi Amidines, isothioureas, and guanidines as nucleophilic catalysts
    James E Taylor
    Department of Chemistry, University of Bath, Claverton Down, Bath, BA2 7AY, UK
    Chem Soc Rev 41:2109-21. 2012
    ..In this respect, amidine and guanidine derived catalysts have been shown to be effective in catalysing aldol reactions, Morita-Baylis-Hillman reactions, conjugate additions, carbonylations, methylations, silylations, and brominations...
  54. pmc Genome-wide analysis of thiourea-modulated salinity stress-responsive transcripts in seeds of Brassica juncea: identification of signalling and effector components of stress tolerance
    A K Srivastava
    Nuclear Agriculture and Biotechnology Division, Bhabha Atomic Research Centre, Mumbai 400085, India
    Ann Bot 106:663-74. 2010
    Abiotic stresses including salinity are the major constraints to crop production. In this regard, the use of thiourea (TU) in imparting salinity-stress tolerance to Indian mustard (Brassica juncea) has been demonstrated earlier...
  55. pmc Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities
    Bianca K Verlinden
    Department of Biochemistry, Faculty of Natural and Agricultural Sciences, University of Pretoria, PO Box x20, Pretoria, 0028, South Africa
    J Med Chem 54:6624-33. 2011
    A series of alkylated (bis)urea and (bis)thiourea polyamine analogues were synthesized and screened for antimalarial activity against chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro...
  56. ncbi Design, synthesis and biological activities of thiourea containing sorafenib analogs as antitumor agents
    Jianwen Yao
    Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan, Shandong 250012, PR China
    Bioorg Med Chem 20:2923-9. 2012
    A novel series of diaryl thiourea containing sorafenib derivatives 9a-t was designed and synthesized. The structures of all the newly synthesized compounds were determined by (1)H NMR, (13)C NMR and HRMS...
  57. ncbi Synthesis, anti-inflammatory and antimicrobial evaluation of novel 1-acetyl-3,5-diaryl-4,5-dihydro (1H) pyrazole derivatives bearing urea, thiourea and sulfonamide moieties
    Ashish P Keche
    Department of Chemistry, Maharashtra Udaygiri Mahavidayla, Udgir, India
    Bioorg Med Chem Lett 22:6611-5. 2012
    ..Compounds 24, 26, 27, 28 and 29 exhibited promising antimicrobial activity at MIC values ranging from 70 to 10 μg/mL against all the selected pathogenic bacteria and fungi...
  58. ncbi H-bonding additives act like Lewis acid catalysts
    Peter R Schreiner
    Institut fur Organische Chemie, Universitat Gottingen, Tammannstrasse 2, 37077, Gottingen, Germany
    Org Lett 4:217-20. 2002
    ..similarities of an exemplary H-bonded complex of an N-acyloxazolidinone with an N,N'-disubstituted electron-poor thiourea and the corresponding Lewis acid complex...
  59. ncbi Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agents
    Wen Yang
    State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China
    Bioorg Med Chem 21:1050-63. 2013
    ..Moreover, the replacement of thiourea skeleton by using benzene ring resulted in the slight diversity of the two series towards specific targets.
  60. ncbi Thiourea derivatives incorporating a hippuric acid moiety: synthesis and evaluation of antibacterial and antifungal activities
    Samir Y Abbas
    Organometallic and Organometalloid Chemistry Department, National Research Centre, El Behous, Dokki, Cairo, Egypt
    Eur J Med Chem 64:111-20. 2013
    New series of thiourea derivatives incorporating a hippuric acid moiety have been synthesized through the reaction of 4-hippuric acid isothiocyanate with various nitrogen nucleophiles such as aliphatic amines, aromatic amines, sulfa drugs,..
  61. ncbi Antifungal efficacy of chitosan and its thiourea derivatives upon the growth of some sugar-beet pathogens
    M Eweis
    Department of Botany, Faculty of Science, Cairo University, Cairo, Egypt
    Int J Biol Macromol 38:1-8. 2006
    Chitosan (CS) was modified by reaction with benzoyl thiocyanate to give a thiourea derivative (TUCS)...
  62. pmc Enantioselective thiourea-catalyzed cationic polycyclizations
    Robert R Knowles
    Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA
    J Am Chem Soc 132:5030-2. 2010
    A new thiourea catalyst is reported for the enantioselective cationic polycyclization of hydroxylactams...
  63. ncbi Human mitochondrial thymidine kinase is selectively inhibited by 3'-thiourea derivatives of beta-thymidine: identification of residues crucial for both inhibition and catalytic activity
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 75:1127-36. 2009
    Substituted 3'-thiourea derivatives of beta-thymidine (dThd) and 5'-thiourea derivatives of alpha-dThd have been evaluated for their inhibitory activity against recombinant human cytosolic dThd kinase-1 (TK-1), human mitochondrial TK-2, ..
  64. pmc Novel class of thiourea compounds that inhibit herpes simplex virus type 1 DNA cleavage and encapsidation: resistance maps to the UL6 gene
    M van Zeijl
    Department of Molecular Biology Virology, Wyeth Ayerst Research, Pearl River, New York 10965, USA
    J Virol 74:9054-61. 2000
    In our search for novel inhibitors of herpes simplex virus type 1 (HSV-1), a new class of thiourea inhibitors was discovered...
  65. ncbi Acetylcholine-induced asynchronous calcium waves in intact human bronchial muscle bundle
    Jiazhen M Dai
    The James Hogg iCAPTURE Center for Cardiovascular and Pulmonary Research, University of British Columbia, and St Paul s Hospital, Room 166, 1081 Burrard Street, Vancouver, BC, V6Z 1Y6 Canada
    Am J Respir Cell Mol Biol 36:600-8. 2007
    ..These findings for the first time demonstrate the occurrence and the role of ACW in excitation-contraction coupling in adult human ASM...
  66. ncbi Studies on the anti-proliferative effects of novel DNA-intercalating bipyridyl-thiourea-Pt(II) complexes against cisplatin-sensitive and -resistant human ovarian cancer cells
    Gaetano Marverti
    Dipartimento di Scienze Biomediche, Sezione di Chimica Biologica, Universita di Modena e Reggio Emilia, Via Campi 287, 41100 Modena, Italy
    J Inorg Biochem 102:699-712. 2008
    Six bipyridyl complexes of platinum(II) with thiourea, with different substituents on thiourea moiety [Pt(bipy)(R,R'NCSNR'',R''')(2)]Cl(2) (bipy=2,2'-bipyridine: R=R'=R''=R''' =H; R=Me, R'=R''=R'''=H; R=n-Bu, R'=R''=R'''=H; R=Et, R'=H, R''..
  67. pmc Osteoporosis regulation by salubrinal through eIF2α mediated differentiation of osteoclast and osteoblast
    Long He
    Korea Research Institute of Bioscience and Biotechnology KRIBB, Korea
    Cell Signal 25:552-60. 2013
    ..In addition, modulation of ATF4 and NFATc1 expressions through eIF2α phosphorylation could be a valuable target for the treatment of osteoporosis...
  68. ncbi N-D-aldopentofuranosyl-N'-[p-(isoamyloxy)phenyl]-thiourea derivatives: potential anti-TB therapeutic agents
    Avraham Liav
    Department of Microbiology, Immunology and Pathology, Colorado State University, 1682 Campus Delivery, Fort Collins, CO 80523, USA
    Bioorg Med Chem Lett 18:2649-51. 2008
    Thiocarlide (THC; N,N'-bis[p-(isoamyloxy)phenyl]-thiourea; also known as isoxyl) has been used in the past as anti-tuberculosis agent...
  69. pmc Mechanism of amido-thiourea catalyzed enantioselective imine hydrocyanation: transition state stabilization via multiple non-covalent interactions
    Stephan J Zuend
    Harvard University, Department of Chemistry and Chemical Biology, Cambridge, Massachusetts 02138, USA
    J Am Chem Soc 131:15358-74. 2009
    An experimental and computational investigation of amido-thiourea promoted imine hydrocyanation has revealed a new and unexpected mechanism of catalysis...
  70. ncbi Differential branchial and renal handling of urea, acetamide and thiourea in the gulf toadfish Opsanus beta: evidence for two transporters
    M D McDonald
    McMaster University, Life Science Building, Hamilton, Ontario, Canada
    J Exp Biol 203:1027-37. 2000
    ..urinary ureteral catheters and injected with an iso-osmotic dose of (14)C-labelled urea analogue (acetamide or thiourea) calculated to bring plasma analogue concentrations close to plasma urea concentrations...
  71. ncbi Salubrinal promotes healing of surgical wounds in rat femurs
    Ping Zhang
    Department of Biomedical Engineering, Indiana University Purdue University Indianapolis, SL220, 723 West Michigan Street, Indianapolis, IN, 46202, USA
    J Bone Miner Metab 30:568-79. 2012
    ..In summary, the results herein demonstrate that subcutaneous administration of salubrinal accelerates healing of surgically generated bone holes through the modulation of eIF2α phosphorylation...
  72. pmc Salubrinal attenuates β-amyloid-induced neuronal death and microglial activation by inhibition of the NF-κB pathway
    Xiumei Huang
    Fujian Provincial Key Laboratory of Neurodegenerative Disease and Aging Research, College of Medicine, Xiamen University, Xiamen, Fujian, China
    Neurobiol Aging 33:1007.e9-17. 2012
    ..This study also suggests that modulation of Aβ-induced NF-κB activation could be a potential therapeutic strategy for Alzheimer's disease...
  73. ncbi Adsorption of platinum(IV) and palladium(II) from aqueous solution by thiourea-modified chitosan microspheres
    Limin Zhou
    Key Laboratory of Nuclear Resources and Environment Ministry of Education, East China Institute of Technology, Xuefu Road No 56, Fuzhou, Jiangxi 344000, PR China
    J Hazard Mater 172:439-46. 2009
    The chitosan microparticles were prepared using the inverse phase emulsion dispersion method and modified with thiourea (TCS)...
  74. ncbi Recovery of silver (I) using a thiourea-modified chitosan resin
    Lin Wang
    Institute of Oceanology, The Chinese Academy of Sciences, Qingdao, 266071, China
    J Hazard Mater 180:577-82. 2010
    ..The resin was synthesized by using O-carboxymethylated chitosan to cross-link a polymeric Schiff's base of thiourea/glutaraldehyde and characterized by IR. Batch method was applied for testing the resin's adsorption behavior...
  75. ncbi (Thio)urea organocatalysis--what can be learnt from anion recognition?
    Zhiguo Zhang
    Institut fur Organische Chemie, Justus Liebig Universitat Giessen, Heinrich Buff Ring 58, D 35392, Giessen, Germany
    Chem Soc Rev 38:1187-98. 2009
    ..In turn, the discovery and mechanistic elucidation of such reactions is likely to improve the understanding of enzyme active sites (108 references)...
  76. ncbi Characteristics of equilibrium, kinetics studies for adsorption of Hg(II), Cu(II), and Ni(II) ions by thiourea-modified magnetic chitosan microspheres
    Limin Zhou
    Key Laboratory of Nuclear Resources and Environment East China Institute of Technology, Ministry of Education, Xuefu Road No 56, Fuzhou, Jiangxi 344000, PR China
    J Hazard Mater 161:995-1002. 2009
    Magnetic chitosan microspheres were prepared and chemically modified with thiourea (TMCS) for adsorption of metal ions...
  77. ncbi Synthesis of some urea and thiourea derivatives of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidine and their antagonistic effects on haloperidol-induced catalepsy and oxidative stress in mice
    Faizul Azam
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Seventh October, Misurata, Libya
    Eur J Med Chem 44:3889-97. 2009
    A series of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7-yl urea and thiourea derivatives were designed and synthesized...
  78. ncbi Rational design and 3D-pharmacophore mapping of 5'-thiourea-substituted alpha-thymidine analogues as mycobacterial TMPK inhibitors
    Carolina H Andrade
    Faculty of Pharmaceutical Sciences, Av Prof Lineu Prestes, 580, University of Sao Paulo, Sao Paulo, 05508 900, Brazil
    J Chem Inf Model 49:1070-8. 2009
    ..RI) 4D-QSAR formalism has been used to develop QSAR models and corresponding 3D-pharmacophores for a set of 5'-thiourea-substituted alpha-thymidine inhibitors...
  79. ncbi Evaluation of nitrification-inhibition measurements
    K Jonsson
    Department of Water and Environmental Engineering, Lund Institute of Technology, P O Box 118, SE 221 00 Lund, Sweden
    Water Sci Technol 43:201-8. 2001
    ..Allyl-thiourea (ATU), methanol, chromium and zinc were used as reference toxicants in combination with different kinds of full-..
  80. pmc KB-R7943, an inhibitor of the reverse Na+ /Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I
    Tatiana Brustovetsky
    Department of Pharmacology and Toxicology Stark Neuroscience Research Institute, Indiana University School of Medicine, Indianapolis, IN, USA
    Br J Pharmacol 162:255-70. 2011
    ..Here, the effects of KB-R7943 on N-methyl-D-aspartate (NMDA) receptors and mitochondrial complex I were tested...
  81. ncbi Bifunctional primary amine-thiourea-TfOH (BPAT·TfOH) as a chiral phase-transfer catalyst: the asymmetric synthesis of dihydropyrimidines
    Yangyun Wang
    State Key Laboratory and Institute of Elemento Organic Chemistry, Nankai University, Tianjin, 300071, China
    Org Biomol Chem 9:3050-4. 2011
    An enantioselective Biginelli reaction has been developed by using a bifunctional primary amine-thiourea-TfOH (BPAT·TfOH) as a chiral phase-transfer catalyst and t-BuNH(2)·TFA as an additive in saturated brine at room temperature...
  82. pmc Specific inhibition of human cytomegalovirus glycoprotein B-mediated fusion by a novel thiourea small molecule
    Thomas R Jones
    Infectious Disease Section, Wyeth Research, Pearl River, New York 10965, USA
    J Virol 78:1289-300. 2004
    ..Furthermore, CFI02 inhibits the cell-cell spread of HCMV. This is the first study of a potent and selective small molecule inhibitor of CMV fusion and cell-cell spread...
  83. ncbi The importance of the oxidative character of doubly charged metal cations in binding neutral bases. [Urea-M]2+ and [thiourea-M]2+ (M = Mg, Ca, Cu) complexes
    Cristina Trujillo
    Departamento de Quimica, C 9, Universidad Autonoma de Madrid, Cantoblanco, 28049 Madrid, Spain
    Phys Chem Chem Phys 10:3229-35. 2008
    ..of the electron density, namely AIM, ELF and NBO, yield coherent descriptions of the bonding in [urea-M](2+) and [thiourea-M](2+) (M = Mg, Ca, Cu) complexes, whose geometries have been optimized at the B3LYP/6-311+G(d,p) level of theory...
  84. ncbi Comparative gene transfer between cationic and thiourea lipoplexes
    Marie Breton
    INSERM, U640, CNRS, UMR8151, Unite de Pharmacologie Chimique et Genetique, Universite Paris Descartes, Faculte de Pharmacie, Paris, France
    J Gene Med 12:45-54. 2010
    ..To further evaluate these lipids, we investigated the internalization process of the thiourea lipoplexes and their intracellular mechanism of transfection versus that of cationic lipoplexes.
  85. ncbi Structure-activity relationship study of the bacterial actin-like protein MreB inhibitors: effects of substitution of benzyl group in S-benzylisothiourea
    Noritaka Iwai
    Department of Bioengineering, Tokyo Institute of Technology, Japan
    Biosci Biotechnol Biochem 71:246-8. 2007
    ..A 2,4-Cl2-derivative was found to be the most effective compound, it was stronger than the original one in Gram-negative rod shaped-bacteria such as Escherichia coli and Salmonella typhimurium...
  86. ncbi The dimethylthiourea-induced attenuation of cisplatin nephrotoxicity is associated with the augmented induction of heat shock proteins
    Takayuki Tsuji
    First Department of Medicine, Hamamatsu University School of Medicine, 1 20 1 Handayama, Higashi ku, Hamamatsu, Shizuoka 431 3192, Japan
    Toxicol Appl Pharmacol 234:202-8. 2009
    ..The findings suggest that DMTU may afford protection against CDDP-induced ARF, partially through the early induction of cytoplasmic HSP60, thereby preventing the Bax-mediated apoptosis in renal tubular cells...
  87. ncbi Involvement of Na(+)/Ca(2+) exchanger in endothelial NO production and endothelium-dependent relaxation
    Jean Christophe Schneider
    Service de Physiologie Explorations Fonctionnelles, Centre Hospitalier Universitaire Cochon, Assistance Publique, Hopitaux de Paris, Universite Paris 5, 75014 Paris, France
    Am J Physiol Heart Circ Physiol 283:H837-44. 2002
    ..These findings confirm the key role of NCX in reverse mode on Ca(2+)-dependent NO production and endothelium-dependent relaxation...
  88. ncbi Functional differences of Na+/Ca2+ exchanger expression in Ca2+ transport system of smooth muscle of guinea pig stomach
    Yasushi Sakai
    Division of Physiolgy, Department of Occupational Therapy, School of Nursing and Rehabilitation Sciences, Yokohama, Japan
    Can J Physiol Pharmacol 83:791-7. 2005
    ..Results documented evidence that NCX2 isoform functionally contributes to Ca2+ extrusion and maintenance of contraction-relaxation cycle in gastric fundus smooth muscle...
  89. pmc Fundamental importance of Na+-Ca2+ exchange for the pacemaking mechanism in guinea-pig sino-atrial node
    Luke Sanders
    University Department of Pharmacology, Mansfield Road, Oxford OX1 3QT, UK
    J Physiol 571:639-49. 2006
    ....
  90. pmc The thioamides methimazole and thiourea inhibit growth of M. avium Subspecies paratuberculosis in culture
    Robert J Greenstein
    Department of Surgery, James J Peters VA Medical Center, Bronx, New York, United States of America
    PLoS ONE 5:e11099. 2010
    ..Because other thioamides treat tuberculosis, leprosy and M. avium complex, we hypothesized that a mode of action of some thioamide anti-thyrotoxicosis medications may include MAP growth inhibition...
  91. ncbi Free radicals generated in yeast by the Salmonella test-negative carcinogens benzene, urethane, thiourea and auramine O
    R J Brennan
    Dept of Cancer Cell Biology, Harvard School of Public Health, Boston, MA 02115 6021, USA
    Mutat Res 403:65-73. 1998
    ..of intracellular free radical species by the diverse Salmonella-negative carcinogens benzene, urethane, thiourea and auramine O...
  92. pmc Direction-independent block of bi-directional Na+/Ca2+ exchange current by KB-R7943 in guinea-pig cardiac myocytes
    J Kimura
    Department of Pharmacology, Fukushima Medical University, School of Medicine, Fukushima 960 1295, Japan
    Br J Pharmacol 128:969-74. 1999
    ..The difference could be attributed to slow dissociation of the drug from the exchanger...
  93. ncbi Highly enantio- and diastereoselective Mannich reactions of glycine Schiff bases with in situ generated N-Boc-imines catalyzed by a cinchona alkaloid thiourea
    Haile Zhang
    The Skaggs Institute for Chemical Biology and the Departments of Chemistry and Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037
    Org Lett 12:708-11. 2010
    ..Imines were generated in situ from bench-stable alpha-amido sulfones. Catalysis mediated by a cinchona alkaloid thiourea provided optically active alpha,beta-diamino acid derivatives with up to 99% ee and near-perfect ..
  94. ncbi Pharmacology of KB-R7943: a Na+-Ca2+ exchange inhibitor
    Md Shah Amran
    Department of Pharmacology, Interdisciplinary Graduate School of Medicine and Engineering, University of Yamanashi, Tamaho, Nakakoma, Yamanashi 409 3898, Japan
    Cardiovasc Drug Rev 21:255-76. 2003
    ....
  95. ncbi Docking and 3D QSAR study of thiourea analogs as potent inhibitors of influenza virus neuraminidase
    Jiaying Sun
    College of Bioengineering, Chongqing University, Chongqing 400044, China
    J Mol Model 16:1809-18. 2010
    Surflex-Dock was applied to study interactions between 30 thiourea analogs and neuraminidase (NA)...
  96. ncbi Development and application of Na+/Ca2+ exchange inhibitors
    Takahiro Iwamoto
    Department of Pharmacology, School of Medicine, Fukuoka University, Fukuoka, Japan
    Mol Cell Biochem 259:157-61. 2004
    ..Here, we summarize pharmacological profiles of KB-R7943 and SEA0400, the molecular mechanism of its action, and its future prospect as a novel pharmaceutical agent...
  97. ncbi Rational design of 5'-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growth
    Ineke Van Daele
    Laboratory for Medicinal Chemistry FFW, University of Gent, Harelbekestraat 72, 9000 Ghent, Belgium
    J Med Chem 50:5281-92. 2007
    ..Several hits identified within a series of 3'-C-branched thiourea-substituted beta-thymidine derivatives inspired us to construct a set of 5'-thiourea-substituted alpha-thymidine ..
  98. ncbi Calcium dynamics and vasomotion in rat mesenteric arteries
    Alexander Schuster
    Cellular Biophysics and Biomechanics Laboratory, Swiss Federal Institute of Technology, Lausanne, Switzerland
    J Cardiovasc Pharmacol 43:539-48. 2004
    ....
  99. ncbi Store-refilling involves both L-type calcium channels and reverse-mode sodium-calcium exchange in airway smooth muscle
    S Hirota
    Firestone Institute for Respiratory Health, St Joseph s Healthcare and Department of Medicine, McMaster University, Hamilton, ON, Canada L8N 4A6
    Eur Respir J 30:269-78. 2007
    ..3, respectively. Taken together, these data suggest that influx of calcium ions through both L-type calcium channels and the reverse-mode of the sodium-calcium exchanger is necessary for complete store-refilling in airway smooth muscle...
  100. ncbi Label-free capacitive immunosensor for microcystin-LR using self-assembled thiourea monolayer incorporated with Ag nanoparticles on gold electrode
    Suchera Loyprasert
    Trace Analysis and Biosensor Research Center, Prince of Songkla University, Hat Yai, Songkhla, Thailand
    Biosens Bioelectron 24:78-86. 2008
    ..Anti-microcystin-LR (anti-MCLR) was immobilized on silver nanoparticles bound to a self-assembled thiourea monolayer. Interaction of anti-MCLR and MCLR were directly detected by capacitance measurement...
  101. ncbi Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents
    Peng Cheng Lv
    State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People s Republic of China
    Bioorg Med Chem 18:4606-14. 2010
    ..Compound C5 showed significant antiproliferative activity against MCF-7 with IC₅₀ of 0.08 μM. Therefore, compound C5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent...

Research Grants64

  1. Mode of Action of Thiorcarlide in Mycobacterium Tuberculosis
    Mary Jackson; Fiscal Year: 2012
    Thiocarlide (THC), a thiourea, inhibits the synthesis of mycolic acids and fatty acids in Mycobacterium tuberculosis (M. tb)...
  2. The molecular basis for a broad range of phenotypes related to hTAS2R38
    Sarah V Lipchock; Fiscal Year: 2012
    ..Individuals expressing the amino acid combination proline- alanine-valine (PAV) find compounds with a thiourea moiety, such as 6-n-propylthiouracil (PROP), to be extremely bitter at low concentrations, whereas individuals ..
  3. Varicella-Zoster Virus Encapsidation Proteins
    Robert J Visalli; Fiscal Year: 2010
    ..N-?-methylbenzyl-N'-aryl thiourea analogs were demonstrated to have specific and potent activity against VZV...
  4. A "radical" approach to tuberculosis infection
    Deborah T Hung; Fiscal Year: 2013
    ..We will use a model of drug tolerance that exploits the ability of thiourea to quench hydroxyl radicals generated by antibiotic exposure, thereby inducing drug tolerance...
  5. Mixed Hydrogen-Bonding Flavin Catalysis for Asymmetric Transformations
    NOAH ZACHARY BURNS; Fiscal Year: 2011
    ..Chiral urea and thiourea hydrogen bond donors have shown broad utility in catalyzing a number of asymmetric carbon-carbon bond forming ..
  6. Development of Small Molecules to Combat Bacterial Biofilms
    Sam Reyes; Fiscal Year: 2012
    ..Samuel Reyes has synthesized sulfonamide, urea, and thiourea derivatives of marine sponge-derived natural products...
  7. Development of Novel Small Molecule Flavivirus Inhibitors
    ERIC W BARKLIS; Fiscal Year: 2010
    We have identified TYT-1 as a novel sultam thiourea inhibitor of West Nile virus (WNV) replication. The compound has a 50% effective concentration (EC50) of 0...
  8. Biomimetic Synthesis of Complex Natural Products
    John A Porco; Fiscal Year: 2013
    ..Jacobsen and coworkers (Harvard University) will seek to identify chiral thiourea photocatalysts for asymmetric photocycloadditions...
  9. Enantioselective Thiourea-Catalyzed Syntheses of beta-Lactones and beta-Lactams
    PAMELA MICHELE TADROSS; Fiscal Year: 2013
    ..Specifically, the thiourea catalyst will mediate the formal [2+2] cycloaddition reaction between ketenes and aldehydes, ketones, and imines...
  10. Asymmetric Prins/aza-Prins Cyclization via Thiourea-Anion Binding Catalysis
    Katrien Brak; Fiscal Year: 2012
    ..Chiral, non-racemic thiourea catalysts have been shown to induce highly enantioselective transformations by binding to the counteranion of ..
  11. MANGANESE (III) BASED OXIDATIVE FREE RADICAL CYCLIZATION
    BARRY SNIDER; Fiscal Year: 2000
    ..will be synthesized by the addition of ammonia to a dienone, condensation of the resulting diamine with a thiourea derivative, and epoxide opening to construct the ticyclic guanidinium core of cylindrospermopsin with control of ..
  12. Enantioselective Thiourea-Catalyzed C-H Functionalization via Hydride Transfer
    DAVID JAMES HARDEE; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): The proposed research is focused on the development of enantioselective thiourea-catalyzed C-H bond functionalization via intramolecular redox reactions...
  13. NON-NITROGEN AND NITROGEN CONTAINING DOPAMINE DRUGS
    Duane Miller; Fiscal Year: 1992
    ..4.To synthesize a set of formamidino, guanidino and thiourea analogs of DA, in order to investigate the overall importance of hydrogen bonding in the interaction of DAergic ..
  14. MICROVASCULAR TRANSPORT IN THE RENAL MEDULLA
    THOMAS PALLONE; Fiscal Year: 2002
    ..Residual osmotic water permeability of AQP1 -/- will be examined for sensitivity to pCMBS and thiourea. The Arrhenius activation energy of remaining pathways will also be determined...
  15. CHEMICAL MODELS OF PRESYNAPTIC NEUROMUSCULAR DISEASE
    WILLIAM ATCHISON; Fiscal Year: 1999
    ..2,4- Dithiobiuret (DTB) is a thiourea derivative which causes a delayed onset neuromuscular weakness that mimics certain human neuromuscular diseases, ..
  16. Enantioselective Synthesis of N-Heterocyclic Rings Using Thiourea-Based Catalysts
    Connor L Martin; Fiscal Year: 2012
    ..The aim of the proposed research is to apply chiral thiourea- based catalysts to the development of new methods for the enantioselective synthesis of nitrogen-containing ..
  17. Stereoselective Synthesis of Ketals using Thiourea-Based Catalysts
    ALAN MICHAEL HYDE; Fiscal Year: 2010
    ..This work may affect several diverse areas of medicine including anticancer, antibacterial, antifungal, and antiviral therapeutics. ..
  18. Mechanisms of Positive Energy Balance in PROP Nontasters
    Kathleen Keller; Fiscal Year: 2009
    Inherited differences in human's ability to taste bitter thiourea compounds, specifically phenylthiocarbamide (PTC) and 6-n-propylthiouracil (PROP), have been studied since 1931. 70% of adults and children in the U.S...
  19. Asymmetric Capture of Carbocations: Novel Access to Benzylic Stereogenicity
    ROBERT KNOWLES; Fiscal Year: 2010
    ..The proposed research will focus on the development of novel thiourea-catalyzed asymmetric, nucleophilic substitution reactions of secondary and tertiary benzylic halides, proceeding ..
  20. CHEMICAL AND ENZYMIC MECHANISM OF THIOCARBAMIDE TOXICITY
    Daniel Doerge; Fiscal Year: 1990
    Man is exposed to toxic derivatives of thiourea (thiocarbamides) in the environment from agricultural, industrial and medicinal sources...
  21. METVAN: A Novel Anticancer Agent
    OSMOND D CRUZ; Fiscal Year: 2003
    ..The knowledge gained from these studies described under Specific Aims 1-2 is expected to facilitate the design of innovative treatment regimens employing METVAN for metastatic breast cancer and brain tumor patients. ..
  22. Vanadocenes as a New Class of Spermicidal Drugs
    OSMOND D CRUZ; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  23. PHI 346: A Novel Dual-Function Microbicide
    OSMOND D CRUZ; Fiscal Year: 2003
    ..Our lead compound, N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (PHI-346), was the most potent, non-cytotoxic, dual-function anti-HIV agent against NNI-sensitive, NNI-resistant, ..
  24. Stampidine: A Novel Broad-Spectrum Anti-HIV Microbicide
    OSMOND D CRUZ; Fiscal Year: 2005
    ..Specific Aims 1 and 2 may provide the foundation for the clinical development of STAMP in Phase II studies as a safe, effective broad-spectrum anti-HIV microbicide without conception-inhibiting functions. ..
  25. Phase II SBIR: WHI-07: A Novel Dual-Function Microbicide
    OSMOND D CRUZ; Fiscal Year: 2005
    ....
  26. FLP-102: Rationally Engineered Antiviral Protein
    OSMOND D CRUZ; Fiscal Year: 2003
    ..The preclinical data on FLP-102 will be essential to further explore the utility of this novel recombinant PAP mutant for Phase II. ..
  27. PHI-443: Novel Non-Spermicidal Anti-HIV Microbicide
    OSMOND D CRUZ; Fiscal Year: 2003
    ..an integrated effort involving synthesis, docking studies, and biological evaluation, we identified a thiophene thiourea non-nucleoside inhibitor (N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea [PHI-443]) with ..
  28. NOVEL CONTRACEPTIVES WITH ANTI-HIV ACTIVITY
    OSMOND D CRUZ; Fiscal Year: 2001
    ..The preclinical data on in vivo efficacies of WHI-05 and WHI-07 will be essential to further explore the utility of these novel drugs for clinical studies in human patients. ..
  29. Thiourea-Catalyzed Nucleophilic Desymmetrization of Meso-Cyclopropanes
    KRISTINE NOLIN; Fiscal Year: 2008
    ..This proposal outlines the development of stereoselective 1,5-functionalization of carbonyls through thiourea catalyzed desymmetrizations of meso-cyclopropanes by nucleophilic ring opening...
  30. AMINOBENZOMORPHAN: POTENTIAL COCAINE ABUSE MEDICATIONS
    Mark Wentland; Fiscal Year: 2009
    ..Radioligand binding, [35S]GTPvS, and mouse antinociceptive assays will be used to characterize new targets pharmacologically. ..
  31. Endotoxin, allergens and pollutants in asthma
    Daniel G Remick; Fiscal Year: 2010
    ..We will also investigate if a new drug approved for the treatment of rheumatoid arthritis will also help prevent asthma. ..
  32. Computational Approach to Ligand Discovery for LPA GPCR and PPAR
    Abby L Parrill; Fiscal Year: 2010
    ..This research can therefore lead to new treatments for cardiovascular disease and cancer. ..
  33. MULTIMODAL DOT-PET MOLECULAR PROBES AND TANDEM SYSTEM
    Joseph P Culver; Fiscal Year: 2010
    ..abstract_text> ..
  34. Development of a high throughput HIV assembly screen
    ERIC W BARKLIS; Fiscal Year: 2010
    ..We propose to develop a high throughput screen that will identify inhibitors of HIV assembly. Such inhibitors will serve as leads in the design of novel drugs for the treatment of AIDS. ..
  35. NATURAL PRODUCT SYNTHESIS THROUGH TEMPLATE DIRECTED C-H
    DUNCAN WARDROP; Fiscal Year: 2003
    ..abstract_text> ..
  36. K + EFFLUX--ROLE IN CA++ HOMEOSTASIS AND EXCITOTOXICITY
    Lech Kiedrowski; Fiscal Year: 2003
    ..These studies may yield a new target for pharmacological intervention to decrease neuronal death following ischemia or hypoglycemia, namely, to prevent excessive K+ loss from the brain during reperfusion. ..
  37. Dietary Omega-3 Fatty Acids and Sudden Cardiac Death
    GEORGE EDWARD BILLMAN; Fiscal Year: 2010
    ..This project will also determine the effectiveness of fish oil supplements in reducing sudden death due to a lethal abnormal heart rhythm after a heart attack. ..
  38. Mechanical response of osteoblasts in 3D matrix
    Hiroki Yokota; Fiscal Year: 2007
    ..Completion of these studies should provide significant insight into the mechanical responses of osteoblasts in a 3D environment, and contribute to developing. q load-induced in vitro connective tissue engineering. ..
  39. PROMOTER- BASED ESTIMATION ANALYSIS
    Hiroki Yokota; Fiscal Year: 2003
    ....
  40. ENVIRONMENTAL LIGHT AND RETINAL MEMBRANE DEVELOPMENT
    Daniel Organisciak; Fiscal Year: 2003
    ..In addition, the time course of the appearance of cytoplasmic cytochrome C and the activation of cellular caspases will be determined by antibody-based techniques, immunocytochemistry and enzymatic analysis. ..
  41. RETROVIRUS STRUCTURAL PROTEIN INTERACTIONS
    Eric Barklis; Fiscal Year: 2001
    ..Cysteines will be substituted into the Gag protein and used in crosslinking studies. This will be used to identify proteins which bind to the Gag major homology region (MHR) and the Fv1 N/B tropism determinant. ..
  42. 2,5 CYCLOHEXADIENONES IN NATURAL PRODUCTS SYNTHESIS
    Mark Wentland; Fiscal Year: 2001
    ....
  43. GENERATION OF THOMSEN-FREIDENREICH-SPECIFIC T CELLS
    Alessandra Franco; Fiscal Year: 2002
    ..Two strategies will be compared: 1) passive immunotherapy by T cell transfer with selected T cell clones; and 2) active vaccination with the glycopeptides and glycolipids to generate a TF-specific T cell response. ..
  44. Extreme Ammonia Tolerance Mechanisms: A Model Vertebrate
    Patrick Walsh; Fiscal Year: 2004
    ..abstract_text> ..
  45. Steroids and Stem Cell in Carcinogenesis
    Doris Benbrook; Fiscal Year: 2004
    ..This research will enhance our understanding of the process of carcinogenesis and chemoprevention, which could ultimately translate into strategies and pharmaceuticals for prevention of cancer. ..
  46. Regulation of Ongoing Inflammation
    Daniel Remick; Fiscal Year: 2009
    ..Successful completion of each of these specific aims will help to determine both the optimal method to regulate ongoing inflammation and the precise mechanisms of how this regulation occurs. ..
  47. Effect of Daily Exercise on Cardiac Autonomic Regulation
    GEORGE BILLMAN; Fiscal Year: 2005
    ..Ventricular contractile responses to Beta1- and Beta2-adrenoceptor stimulation will be examined in vivo by echocardiography and in vitro by single cell fluorescence microscopy/video edge detection. ..
  48. Synthesis through N-Acylnitrenium Ion Cyclization
    DUNCAN WARDROP; Fiscal Year: 2006
    ..abstract_text> ..
  49. Novel Monomolecular Multi Modality Imaging Agents
    Samuel Achilefu; Fiscal Year: 2006
    ..Successful completion of this study will result in the development of at least one MOMIA for translational research and eventual clinical use. ..
  50. ADVANCES IN OPTICS FOR BIOTECHNOLOGY, MEDICINE AND SURGERY CONFERENCE
    Samuel Achilefu; Fiscal Year: 2007
    ..unreadable] Aim 4: To promote interaction between the invited scientists and participating students, and to enable [unreadable] collaborations. [unreadable] [unreadable] [unreadable]..
  51. Tissue-Specific Optical Imaging Agents and Methods
    Samuel Achilefu; Fiscal Year: 2007
    ..Products of this study will also be made available to other investigators interested in molecular-probe- mediated optical imaging and related medical/pharmaceutical applications. ..
  52. Immunopathology of Sepsis
    Daniel Remick; Fiscal Year: 2007
    ..Successful completion our goals will define both basic mechanisms of disease and potential targets for therapeutic intervention. ..
  53. PLASTICITY AT A CRAYFISH NEUROMUSCULAR SYNAPSE
    Jen Wei Lin; Fiscal Year: 2003
    ....
  54. iNOS Posttranslational Regulation in Cardiac Rejection
    GALEN PIEPER; Fiscal Year: 2009
    ..A better understanding of this molecular process may lead to better strategies to prevent injury cardiac cells in these patients. ..
  55. Functional Organization of the Myelin Membrane
    Christopher Taylor; Fiscal Year: 2003
    ..in forming rafts in myelin, 3) provide a more complete understanding of the organization of proteins and lipids in myelin as well as identify potential targets for the therapeutic intervention in many myelin related disorders/diseases ..
  56. Rexinoid Synergy in Prostate Cancer Apoptosis
    Marcia Dawson; Fiscal Year: 2009
    ..We anticipate that our results will provide a more effective and less systemically toxic means of enhancing the efficacy of chemotherapeutic agents currently used to treat prostate cancer. ..
  57. Release of Apoptogenic Proteins from Brain Mitochondria
    Nickolay Brustovetsky; Fiscal Year: 2009
    ..abstract_text> ..
  58. Malaria PfCRT Transporter: Structure, Function, Sorting
    MYLES AKABAS; Fiscal Year: 2006
    ..It is the current lack of such an assay and the fact that this is a high risk search that has motivated us to apply for an R21 grant, which is exploratory in nature, rather than an RO1. ..
  59. Small GTPases and Lung Endothelial Apoptosis
    Sharon Rounds; Fiscal Year: 2009
    ..In addition, understanding of apoptosis may provide clues to treatment of lung diseases dependent upon abnormal endothelial proliferation, such as Pulmonary Arterial Hypertension and cancer. ..
  60. SHORT TERM TRAINING FOR MINORITY STUDENTS
    Sharon Rounds; Fiscal Year: 2006
    ..We present results of our previous experience showing that of students trained thus far, 45 percent have gone on to MD, PhD, or MD/PhD training programs. ..
  61. Analysis of Sin Nombre virus inhibition in lung cells
    Eric Barklis; Fiscal Year: 2005
    ..We believe that these exploratory studies have a high probability of leading to more efficient treatment of hantavirus-mediated pulmonary failure. ..