Genomes and Genes
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.
Publications299 found, 100 shown here
- A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stressMichael 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...
- Synthesis, spectroscopic properties and antipathogenic activity of new thiourea derivativesCarmen 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 ..
- Autophagy regulates endoplasmic reticulum stress in ischemic preconditioningRui 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...
- 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 pathwayGa 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...
- Improved ligand-protein binding affinity predictions using multiple binding modesEva 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...
- SPA0355, a thiourea analogue, inhibits inflammatory responses and joint destruction in fibroblast-like synoviocytes and mice with collagen-induced arthritisY 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...
- Selective inhibition of eukaryotic translation initiation factor 2 alpha dephosphorylation potentiates fatty acid-induced endoplasmic reticulum stress and causes pancreatic beta-cell dysfunction and apoptosisMiriam 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...
- (Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulatorsShiv 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...
- Deficiency of αB crystallin augments ER stress-induced apoptosis by enhancing mitochondrial dysfunctionGuorui 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...
- Synthesis and antiviral activities of chiral thiourea derivatives containing an alpha-aminophosphonate moietyMei 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.
- Attractive noncovalent interactions in asymmetric catalysis: links between enzymes and small molecule catalystsRobert 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...
- Synergistic apoptosis induction in leukemic cells by the phosphatase inhibitor salubrinal and proteasome inhibitorsHannes C A Drexler
Department of Vascular Cell Biology, Max Planck Institute for Molecular Biomedicine, Muenster, Germany
PLoS ONE 4:e4161. 2009....
- Superoxide, H2O2, and iron are required for TNF-alpha-induced MCP-1 gene expression in endothelial cells: role of Rac1 and NADPH oxidaseXi 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...
- A pharmacoproteomic approach implicates eukaryotic elongation factor 2 kinase in ER stress-induced cell deathM 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...
- Effect of SEA0400, a novel inhibitor of sodium-calcium exchanger, on myocardial ionic currentsHikaru 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...
- Sex differences in the effects of inherited bitter thiourea sensitivity on body weight in 4-6-year-old childrenKathleen 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...
- MreB drives de novo rod morphogenesis in Caulobacter crescentus via remodeling of the cell wallConstantin 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...
- Isothioureas: potent inhibitors of nitric oxide synthases with variable isoform selectivityG J Southan
William Harvey Research Institute, St Bartholomew s Hospital Medical College, London
Br J Pharmacol 114:510-6. 1995....
- Induction of autophagic cell death by a novel molecule is increased by hypoxiaMarco 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...
- 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 metalloenzymesMichael 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...
- Development of chiral thiourea catalysts and its application to asymmetric catalytic reactionsYoshiji Takemoto
Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida, Sakyo ku, Kyoto 606 8501, Japan
Chem Pharm Bull (Tokyo) 58:593-601. 2010We 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 ..
- Na+-Ca2+ exchanger contributes to Ca2+ extrusion in ATP-stimulated endothelium of intact rat aortaRoberto 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...
- Fluorescence enhancement of coumarin thiourea derivatives by Hg2+, Ag+, and silver nanoparticlesAhmed 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 ..
- Synthesis, characterization and biological evaluation of some thiourea derivatives bearing benzothiazole moiety as potential antimicrobial and anticancer agentsSohail Saeed
Department of Chemistry, Research Complex, Allama Iqbal Open University, Islamabad, Pakistan
Eur J Med Chem 45:1323-31. 2010Five series of thiourea derivatives bearing benzothiazole moiety (20 compounds) were efficiently synthesized and evaluated for antimicrobial and anticancer activities...
- Synthesis and evaluation of a thiourea-modified chitosan derivative applied for adsorption of Hg(II) from synthetic wastewaterLin Wang
Institute of Oceanology, The Chinese Academy of Sciences, Qingdao 266071, China
Int J Biol Macromol 46:524-8. 2010In 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...
- Therapeutic potential of novel Na+-Ca2+ exchange inhibitors in attenuating ischemia-reperfusion injuryCandace 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...
- Synthesis and microbiological activity of thiourea derivatives of 4-azatricyclo[184.108.40.206(2,6)]undec-8-ene-3,5-dioneMarta Struga
Medical University, Department of Medical Chemistry, 3 Oczki Str, 02 007 Warsaw, Poland
Arch Pharm Res 33:47-54. 2010A series of thiourea derivatives of 4-azatricyclo[220.127.116.11(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...
- Antitumor activity of a new N-substituted thiourea derivative, an EGFR signaling-targeted inhibitor against a panel of human lung cancer cell linesXishan 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...
- Theoretical studies on the bifunctionality of chiral thiourea-based organocatalysts: competing routes to C-C bond formationAndrea 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. 2006The 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...
- 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 receptorLei 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, ..
- Transformation of herbicide propachlor by an agrochemical thioureaWei 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 ..
- The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporterJ 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. 2007The 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...
- Organocatalytic claisen rearrangement: theory and experimentMartin 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...
- Dissolving cellulose in a NaOH/thiourea aqueous solution: a topochemical investigationLifeng 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...
- Synthesis of acyl thiourea derivatives of chitosan and their antimicrobial activities in vitroZhimei Zhong
Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China
Carbohydr Res 343:566-70. 2008Three different acyl thiourea derivatives of chitosan (CS) were synthesized and their structures were characterized by FT-IR spectroscopy and elemental analysis...
- Synthesis, characterization and in vitro antibacterial activity of thiourea and urea derivatives of steroidsSalman Ahmad Khan
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India
Eur J Med Chem 43:2272-7. 2008Some 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...
- Fluorescent labelled thiourea-bridged glycodendronsPavel 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...
- Asymmetric 1,4-addition of oxazolones to nitroalkenes by bifunctional cinchona alkaloid thiourea organocatalysts: synthesis of alpha,alpha-disubstituted alpha-amino acidsJosé 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 ..
- Thiourea modulates the expression and activity profile of mtATPase under salinity stress in seeds of Brassica junceaA 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...
- Synthesis and antitumor activity of optically active thiourea and their 2-aminobenzothiazole derivatives: a novel class of anticancer agentsS 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...
- Weak Brønsted acid-thiourea co-catalysis: enantioselective, catalytic protio-Pictet-Spengler reactionsRebekka S Klausen
Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA
Org Lett 11:887-90. 2009The development of one-pot imine formation and asymmetric Pictet-Spengler reactions cocatalyzed by a chiral thiourea and benzoic acid is described...
- Novel broad-spectrum thiourea non-nucleoside inhibitors for the prevention of mucosal HIV transmissionOSMOND 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...
- Synthesis and biological activity of substituted urea and thiourea derivatives containing 1,2,4-triazole moietiesBedia Kocyigit-Kaymakcioglu
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Haydarpasa 34668, Istanbul, Turkey
Molecules 18:3562-76. 2013A series of novel thiourea and urea derivatives containing 1,2,4-triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity...
- Disubstituted thiourea derivatives and their activity on CNS: synthesis and biological evaluationJoanna Stefanska
Department of Pharmaceutical Microbiology, Medical University, 02 007 Warsaw, Poland
Eur J Med Chem 55:205-13. 2012A 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)...
- Isothiourea-catalysed asymmetric C-acylation of silyl ketene acetalsPhilip 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)...
- Synthesis and bioactivity of pyrazole acyl thiourea derivativesJian 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. 2012Sixteen novel pyrazole acyl thiourea derivatives 6 were synthesized from monomethylhydrazine (phenylhydrazine) and ethyl acetoacetate...
- 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. 2011b>Thiourea (TU) has been found to enhance the stress tolerance of plants in our earlier field trials...
- A novel pyrimidine derivatives with aryl urea, thiourea and sulfonamide moieties: synthesis, anti-inflammatory and antimicrobial evaluationAshish 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...
- Selective inclusion of PO4(3-) within persistent dimeric capsules of a tris(thiourea) receptor and evidence of cation/solvent sealed unimolecular capsulesSandeep Kumar Dey
Department of Chemistry, Indian Institute of Technology Guwahati, Assam 781 03, India
Dalton Trans 41:8960-72. 2012A 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 ..
- Design and synthesis of thiourea derivatives containing a benzo[5,6]cyclohepta[1,2-b]pyridine moiety as potential antitumor and anti-inflammatory agentsWukun Liu
Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, Nanjing, PR China
Bioorg Med Chem Lett 22:2701-4. 2012b>Thiourea derivatives (6a-e) were developed and screened for antitumor and anti-inflammatory activity...
- N-(3-Acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea derivatives as potent vanilloid receptor agonists and analgesicsJ Lee
Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, South Korea
Bioorg Med Chem 9:19-32. 2001A 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...
- Thiourea compound AW00178 sensitizes human H1299 lung carcinoma cells to TRAIL-mediated apoptosisByung 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...
- Amidines, isothioureas, and guanidines as nucleophilic catalystsJames 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...
- Genome-wide analysis of thiourea-modulated salinity stress-responsive transcripts in seeds of Brassica juncea: identification of signalling and effector components of stress toleranceA K Srivastava
Nuclear Agriculture and Biotechnology Division, Bhabha Atomic Research Centre, Mumbai 400085, India
Ann Bot 106:663-74. 2010Abiotic 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...
- Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activitiesBianca 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. 2011A 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...
- Design, synthesis and biological activities of thiourea containing sorafenib analogs as antitumor agentsJianwen 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. 2012A 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...
- Synthesis, anti-inflammatory and antimicrobial evaluation of novel 1-acetyl-3,5-diaryl-4,5-dihydro (1H) pyrazole derivatives bearing urea, thiourea and sulfonamide moietiesAshish 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...
- H-bonding additives act like Lewis acid catalystsPeter 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...
- Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agentsWen 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.
- Thiourea derivatives incorporating a hippuric acid moiety: synthesis and evaluation of antibacterial and antifungal activitiesSamir Y Abbas
Organometallic and Organometalloid Chemistry Department, National Research Centre, El Behous, Dokki, Cairo, Egypt
Eur J Med Chem 64:111-20. 2013New 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,..
- Antifungal efficacy of chitosan and its thiourea derivatives upon the growth of some sugar-beet pathogensM Eweis
Department of Botany, Faculty of Science, Cairo University, Cairo, Egypt
Int J Biol Macromol 38:1-8. 2006Chitosan (CS) was modified by reaction with benzoyl thiocyanate to give a thiourea derivative (TUCS)...
- Enantioselective thiourea-catalyzed cationic polycyclizationsRobert R Knowles
Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA
J Am Chem Soc 132:5030-2. 2010A new thiourea catalyst is reported for the enantioselective cationic polycyclization of hydroxylactams...
- Human mitochondrial thymidine kinase is selectively inhibited by 3'-thiourea derivatives of beta-thymidine: identification of residues crucial for both inhibition and catalytic activityJan Balzarini
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
Mol Pharmacol 75:1127-36. 2009Substituted 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, ..
- Novel class of thiourea compounds that inhibit herpes simplex virus type 1 DNA cleavage and encapsidation: resistance maps to the UL6 geneM van Zeijl
Department of Molecular Biology Virology, Wyeth Ayerst Research, Pearl River, New York 10965, USA
J Virol 74:9054-61. 2000In our search for novel inhibitors of herpes simplex virus type 1 (HSV-1), a new class of thiourea inhibitors was discovered...
- Acetylcholine-induced asynchronous calcium waves in intact human bronchial muscle bundleJiazhen 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...
- Studies on the anti-proliferative effects of novel DNA-intercalating bipyridyl-thiourea-Pt(II) complexes against cisplatin-sensitive and -resistant human ovarian cancer cellsGaetano 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. 2008Six 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''..
- Osteoporosis regulation by salubrinal through eIF2α mediated differentiation of osteoclast and osteoblastLong 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...
- N-D-aldopentofuranosyl-N'-[p-(isoamyloxy)phenyl]-thiourea derivatives: potential anti-TB therapeutic agentsAvraham 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. 2008Thiocarlide (THC; N,N'-bis[p-(isoamyloxy)phenyl]-thiourea; also known as isoxyl) has been used in the past as anti-tuberculosis agent...
- Mechanism of amido-thiourea catalyzed enantioselective imine hydrocyanation: transition state stabilization via multiple non-covalent interactionsStephan J Zuend
Harvard University, Department of Chemistry and Chemical Biology, Cambridge, Massachusetts 02138, USA
J Am Chem Soc 131:15358-74. 2009An experimental and computational investigation of amido-thiourea promoted imine hydrocyanation has revealed a new and unexpected mechanism of catalysis...
- Differential branchial and renal handling of urea, acetamide and thiourea in the gulf toadfish Opsanus beta: evidence for two transportersM 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...
- Salubrinal promotes healing of surgical wounds in rat femursPing 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...
- Salubrinal attenuates β-amyloid-induced neuronal death and microglial activation by inhibition of the NF-κB pathwayXiumei 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...
- Adsorption of platinum(IV) and palladium(II) from aqueous solution by thiourea-modified chitosan microspheresLimin 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. 2009The chitosan microparticles were prepared using the inverse phase emulsion dispersion method and modified with thiourea (TCS)...
- Recovery of silver (I) using a thiourea-modified chitosan resinLin 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...
- (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)...
- Characteristics of equilibrium, kinetics studies for adsorption of Hg(II), Cu(II), and Ni(II) ions by thiourea-modified magnetic chitosan microspheresLimin 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. 2009Magnetic chitosan microspheres were prepared and chemically modified with thiourea (TMCS) for adsorption of metal ions...
- 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 miceFaizul Azam
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Seventh October, Misurata, Libya
Eur J Med Chem 44:3889-97. 2009A series of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7-yl urea and thiourea derivatives were designed and synthesized...
- Rational design and 3D-pharmacophore mapping of 5'-thiourea-substituted alpha-thymidine analogues as mycobacterial TMPK inhibitorsCarolina 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...
- Evaluation of nitrification-inhibition measurementsK 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-..
- KB-R7943, an inhibitor of the reverse Na+ /Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex ITatiana 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...
- Bifunctional primary amine-thiourea-TfOH (BPAT·TfOH) as a chiral phase-transfer catalyst: the asymmetric synthesis of dihydropyrimidinesYangyun Wang
State Key Laboratory and Institute of Elemento Organic Chemistry, Nankai University, Tianjin, 300071, China
Org Biomol Chem 9:3050-4. 2011An 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...
- Specific inhibition of human cytomegalovirus glycoprotein B-mediated fusion by a novel thiourea small moleculeThomas 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...
- 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) complexesCristina 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...
- Comparative gene transfer between cationic and thiourea lipoplexesMarie 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.
- Structure-activity relationship study of the bacterial actin-like protein MreB inhibitors: effects of substitution of benzyl group in S-benzylisothioureaNoritaka 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...
- The dimethylthiourea-induced attenuation of cisplatin nephrotoxicity is associated with the augmented induction of heat shock proteinsTakayuki 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...
- Involvement of Na(+)/Ca(2+) exchanger in endothelial NO production and endothelium-dependent relaxationJean 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...
- Functional differences of Na+/Ca2+ exchanger expression in Ca2+ transport system of smooth muscle of guinea pig stomachYasushi 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...
- Fundamental importance of Na+-Ca2+ exchange for the pacemaking mechanism in guinea-pig sino-atrial nodeLuke Sanders
University Department of Pharmacology, Mansfield Road, Oxford OX1 3QT, UK
J Physiol 571:639-49. 2006....
- The thioamides methimazole and thiourea inhibit growth of M. avium Subspecies paratuberculosis in cultureRobert 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...
- Free radicals generated in yeast by the Salmonella test-negative carcinogens benzene, urethane, thiourea and auramine OR 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...
- Direction-independent block of bi-directional Na+/Ca2+ exchange current by KB-R7943 in guinea-pig cardiac myocytesJ 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...
- Highly enantio- and diastereoselective Mannich reactions of glycine Schiff bases with in situ generated N-Boc-imines catalyzed by a cinchona alkaloid thioureaHaile 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 ..
- Pharmacology of KB-R7943: a Na+-Ca2+ exchange inhibitorMd 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....
- Docking and 3D QSAR study of thiourea analogs as potent inhibitors of influenza virus neuraminidaseJiaying Sun
College of Bioengineering, Chongqing University, Chongqing 400044, China
J Mol Model 16:1809-18. 2010Surflex-Dock was applied to study interactions between 30 thiourea analogs and neuraminidase (NA)...
- Development and application of Na+/Ca2+ exchange inhibitorsTakahiro 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...
- Rational design of 5'-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growthIneke 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 ..
- Calcium dynamics and vasomotion in rat mesenteric arteriesAlexander Schuster
Cellular Biophysics and Biomechanics Laboratory, Swiss Federal Institute of Technology, Lausanne, Switzerland
J Cardiovasc Pharmacol 43:539-48. 2004....
- Store-refilling involves both L-type calcium channels and reverse-mode sodium-calcium exchange in airway smooth muscleS 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...
- Label-free capacitive immunosensor for microcystin-LR using self-assembled thiourea monolayer incorporated with Ag nanoparticles on gold electrodeSuchera 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...
- Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agentsPeng 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...
- Mode of Action of Thiorcarlide in Mycobacterium TuberculosisMary Jackson; Fiscal Year: 2012Thiocarlide (THC), a thiourea, inhibits the synthesis of mycolic acids and fatty acids in Mycobacterium tuberculosis (M. tb)...
- The molecular basis for a broad range of phenotypes related to hTAS2R38Sarah 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 ..
- Varicella-Zoster Virus Encapsidation ProteinsRobert J Visalli; Fiscal Year: 2010..N-?-methylbenzyl-N'-aryl thiourea analogs were demonstrated to have specific and potent activity against VZV...
- A "radical" approach to tuberculosis infectionDeborah 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...
- Mixed Hydrogen-Bonding Flavin Catalysis for Asymmetric TransformationsNOAH 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 ..
- Development of Small Molecules to Combat Bacterial BiofilmsSam Reyes; Fiscal Year: 2012..Samuel Reyes has synthesized sulfonamide, urea, and thiourea derivatives of marine sponge-derived natural products...
- Development of Novel Small Molecule Flavivirus InhibitorsERIC W BARKLIS; Fiscal Year: 2010We 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...
- Biomimetic Synthesis of Complex Natural ProductsJohn A Porco; Fiscal Year: 2013..Jacobsen and coworkers (Harvard University) will seek to identify chiral thiourea photocatalysts for asymmetric photocycloadditions...
- Enantioselective Thiourea-Catalyzed Syntheses of beta-Lactones and beta-LactamsPAMELA MICHELE TADROSS; Fiscal Year: 2013..Specifically, the thiourea catalyst will mediate the formal [2+2] cycloaddition reaction between ketenes and aldehydes, ketones, and imines...
- Asymmetric Prins/aza-Prins Cyclization via Thiourea-Anion Binding CatalysisKatrien Brak; Fiscal Year: 2012..Chiral, non-racemic thiourea catalysts have been shown to induce highly enantioselective transformations by binding to the counteranion of ..
- MANGANESE (III) BASED OXIDATIVE FREE RADICAL CYCLIZATIONBARRY 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 ..
- Enantioselective Thiourea-Catalyzed C-H Functionalization via Hydride TransferDAVID JAMES HARDEE; Fiscal Year: 2013DESCRIPTION (provided by applicant): The proposed research is focused on the development of enantioselective thiourea-catalyzed C-H bond functionalization via intramolecular redox reactions...
- NON-NITROGEN AND NITROGEN CONTAINING DOPAMINE DRUGSDuane 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 ..
- MICROVASCULAR TRANSPORT IN THE RENAL MEDULLATHOMAS 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...
- CHEMICAL MODELS OF PRESYNAPTIC NEUROMUSCULAR DISEASEWILLIAM 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, ..
- Enantioselective Synthesis of N-Heterocyclic Rings Using Thiourea-Based CatalystsConnor 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 ..
- Stereoselective Synthesis of Ketals using Thiourea-Based CatalystsALAN MICHAEL HYDE; Fiscal Year: 2010..This work may affect several diverse areas of medicine including anticancer, antibacterial, antifungal, and antiviral therapeutics. ..
- Mechanisms of Positive Energy Balance in PROP NontastersKathleen Keller; Fiscal Year: 2009Inherited 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...
- Asymmetric Capture of Carbocations: Novel Access to Benzylic StereogenicityROBERT 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 ..
- CHEMICAL AND ENZYMIC MECHANISM OF THIOCARBAMIDE TOXICITYDaniel Doerge; Fiscal Year: 1990Man is exposed to toxic derivatives of thiourea (thiocarbamides) in the environment from agricultural, industrial and medicinal sources...
- METVAN: A Novel Anticancer AgentOSMOND 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. ..
- Vanadocenes as a New Class of Spermicidal DrugsOSMOND D CRUZ; Fiscal Year: 2007..unreadable] [unreadable] [unreadable]..
- PHI 346: A Novel Dual-Function MicrobicideOSMOND 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, ..
- Stampidine: A Novel Broad-Spectrum Anti-HIV MicrobicideOSMOND 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. ..
- Phase II SBIR: WHI-07: A Novel Dual-Function MicrobicideOSMOND D CRUZ; Fiscal Year: 2005....
- FLP-102: Rationally Engineered Antiviral ProteinOSMOND 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. ..
- PHI-443: Novel Non-Spermicidal Anti-HIV MicrobicideOSMOND 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 ..
- NOVEL CONTRACEPTIVES WITH ANTI-HIV ACTIVITYOSMOND 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. ..
- Thiourea-Catalyzed Nucleophilic Desymmetrization of Meso-CyclopropanesKRISTINE 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...
- AMINOBENZOMORPHAN: POTENTIAL COCAINE ABUSE MEDICATIONSMark Wentland; Fiscal Year: 2009..Radioligand binding, [35S]GTPvS, and mouse antinociceptive assays will be used to characterize new targets pharmacologically. ..
- Endotoxin, allergens and pollutants in asthmaDaniel 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. ..
- Computational Approach to Ligand Discovery for LPA GPCR and PPARAbby L Parrill; Fiscal Year: 2010..This research can therefore lead to new treatments for cardiovascular disease and cancer. ..
- MULTIMODAL DOT-PET MOLECULAR PROBES AND TANDEM SYSTEMJoseph P Culver; Fiscal Year: 2010..abstract_text> ..
- Development of a high throughput HIV assembly screenERIC 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. ..
- NATURAL PRODUCT SYNTHESIS THROUGH TEMPLATE DIRECTED C-HDUNCAN WARDROP; Fiscal Year: 2003..abstract_text> ..
- K + EFFLUX--ROLE IN CA++ HOMEOSTASIS AND EXCITOTOXICITYLech 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. ..
- Dietary Omega-3 Fatty Acids and Sudden Cardiac DeathGEORGE 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. ..
- Mechanical response of osteoblasts in 3D matrixHiroki 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. ..
- PROMOTER- BASED ESTIMATION ANALYSISHiroki Yokota; Fiscal Year: 2003....
- ENVIRONMENTAL LIGHT AND RETINAL MEMBRANE DEVELOPMENTDaniel 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. ..
- RETROVIRUS STRUCTURAL PROTEIN INTERACTIONSEric 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. ..
- 2,5 CYCLOHEXADIENONES IN NATURAL PRODUCTS SYNTHESISMark Wentland; Fiscal Year: 2001....
- GENERATION OF THOMSEN-FREIDENREICH-SPECIFIC T CELLSAlessandra 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. ..
- Extreme Ammonia Tolerance Mechanisms: A Model VertebratePatrick Walsh; Fiscal Year: 2004..abstract_text> ..
- Steroids and Stem Cell in CarcinogenesisDoris 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. ..
- Regulation of Ongoing InflammationDaniel 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. ..
- Effect of Daily Exercise on Cardiac Autonomic RegulationGEORGE 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. ..
- Synthesis through N-Acylnitrenium Ion CyclizationDUNCAN WARDROP; Fiscal Year: 2006..abstract_text> ..
- Novel Monomolecular Multi Modality Imaging AgentsSamuel 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. ..
- ADVANCES IN OPTICS FOR BIOTECHNOLOGY, MEDICINE AND SURGERY CONFERENCESamuel 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]..
- Tissue-Specific Optical Imaging Agents and MethodsSamuel 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. ..
- Immunopathology of SepsisDaniel Remick; Fiscal Year: 2007..Successful completion our goals will define both basic mechanisms of disease and potential targets for therapeutic intervention. ..
- PLASTICITY AT A CRAYFISH NEUROMUSCULAR SYNAPSEJen Wei Lin; Fiscal Year: 2003....
- iNOS Posttranslational Regulation in Cardiac RejectionGALEN PIEPER; Fiscal Year: 2009..A better understanding of this molecular process may lead to better strategies to prevent injury cardiac cells in these patients. ..
- Functional Organization of the Myelin MembraneChristopher 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 ..
- Rexinoid Synergy in Prostate Cancer ApoptosisMarcia 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. ..
- Release of Apoptogenic Proteins from Brain MitochondriaNickolay Brustovetsky; Fiscal Year: 2009..abstract_text> ..
- Malaria PfCRT Transporter: Structure, Function, SortingMYLES 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. ..
- Small GTPases and Lung Endothelial ApoptosisSharon 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. ..
- SHORT TERM TRAINING FOR MINORITY STUDENTSSharon 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. ..
- Analysis of Sin Nombre virus inhibition in lung cellsEric 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. ..