thiadiazoles

Summary

Top Publications

  1. ncbi Levels and immunolocalization of endogenous cytokinins in thidiazuron-induced shoot organogenesis in carnation
    Eva Casanova
    Unitat de Fisiologia Vegetal, Departament de Biologia Vegetal, Facultat de Biologia, Universitat de Barcelona, Avgda Diagonal 645, E 08028 Barcelona, Spain
    J Plant Physiol 161:95-104. 2004
  2. ncbi Anticancer, neuroprotective activities and computational studies of 2-amino-1,3,4-thiadiazole based compound
    Wojciech Rzeski
    Department of Virology and Immunology, Institute of Microbiology and Biotechnology, Maria Curie Skłodowska University, Lublin, Poland
    Bioorg Med Chem 15:3201-7. 2007
  3. pmc GSK3beta promotes apoptosis after renal ischemic injury
    Zhiyong Wang
    Evans Biomedical Research Center, Renal Section, Room 546, 650 Albany Street, Boston, MA 02118 2518, USA
    J Am Soc Nephrol 21:284-94. 2010
  4. ncbi GSK-3beta inhibitors attenuate the organ injury/dysfunction caused by endotoxemia in the rat
    Laura Dugo
    Centre for Experimental Medicine, Nephrology and Critical Care Medicine, The William Harvey Research Institute, St Bartholomew s and the Royal London School of Medicine and Dentistry, Charterhouse Square, London, UK
    Crit Care Med 33:1903-12. 2005
  5. pmc Inhibition of gamma-secretase activity inhibits tumor progression in a mouse model of pancreatic ductal adenocarcinoma
    Ruben Plentz
    Department of Medicine, Massachusetts General Hospital Cancer Center, Harvard Medical School, Boston, Massachusetts 02114, USA
    Gastroenterology 136:1741-9.e6. 2009
  6. pmc Inhibiting glycogen synthase kinase-3 reduces endotoxaemic acute renal failure by down-regulating inflammation and renal cell apoptosis
    Y Wang
    Department of Microbiology and Immunology, National Cheng Kung University Medical College, Tainan 701, Taiwan
    Br J Pharmacol 157:1004-13. 2009
  7. doi 5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone
    Inga Cikotiene
    Laboratory of Biothermodynamics and Drug Design, Insitute of Biotechnology, Graiciuno 8, Vilnius LT 02241, Lithuania
    Bioorg Med Chem Lett 19:1089-92. 2009
  8. pmc Store-operated Ca(2+) entry (SOCE) contributes to normal skeletal muscle contractility in young but not in aged skeletal muscle
    Angela M Thornton
    Department of Physiology and Biophysics, Robert Wood Johnson Medical School, Piscataway, NJ 08854, USA
    Aging (Albany NY) 3:621-34. 2011
  9. ncbi Synthesis, fungicidal activity, and 3D-QSAR of pyridazinone-substituted 1,3,4-oxadiazoles and 1,3,4-thiadiazoles
    Xia Juan Zou
    State Key Laboratory for Structural Chemistry Studies of Stable and Unstable Species, Institute of Physical Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing, P R China, 100871
    J Agric Food Chem 50:3757-60. 2002
  10. ncbi Glycogen synthase kinase-3beta inhibitors protect against the organ injury and dysfunction caused by hemorrhage and resuscitation
    Laura Dugo
    Centre of Experimental Medicine, Nephrology and Critical Care, The William Harvey Research Institute, St Bartholomew s and the Royal London School of Medicine and Dentistry, Charterhouse Square, London EC1M 6BQ, UK
    Shock 25:485-91. 2006

Detail Information

Publications192 found, 100 shown here

  1. ncbi Levels and immunolocalization of endogenous cytokinins in thidiazuron-induced shoot organogenesis in carnation
    Eva Casanova
    Unitat de Fisiologia Vegetal, Departament de Biologia Vegetal, Facultat de Biologia, Universitat de Barcelona, Avgda Diagonal 645, E 08028 Barcelona, Spain
    J Plant Physiol 161:95-104. 2004
    ..To our knowledge, this study is the first to evaluate the effect of TDZ on endogenous phytohormones in an organogenic process...
  2. ncbi Anticancer, neuroprotective activities and computational studies of 2-amino-1,3,4-thiadiazole based compound
    Wojciech Rzeski
    Department of Virology and Immunology, Institute of Microbiology and Biotechnology, Maria Curie Skłodowska University, Lublin, Poland
    Bioorg Med Chem 15:3201-7. 2007
    ..To determine probability of tautomeric transition and indicate potential sites of interactions of FABT molecule with the receptor, quantum-chemical calculations with the ab initio Hartree-Fock model were made...
  3. pmc GSK3beta promotes apoptosis after renal ischemic injury
    Zhiyong Wang
    Evans Biomedical Research Center, Renal Section, Room 546, 650 Albany Street, Boston, MA 02118 2518, USA
    J Am Soc Nephrol 21:284-94. 2010
    ..Taken together, GSK3beta-mediated Bax activation induces apoptosis and tubular damage that contribute to acute ischemic kidney injury...
  4. ncbi GSK-3beta inhibitors attenuate the organ injury/dysfunction caused by endotoxemia in the rat
    Laura Dugo
    Centre for Experimental Medicine, Nephrology and Critical Care Medicine, The William Harvey Research Institute, St Bartholomew s and the Royal London School of Medicine and Dentistry, Charterhouse Square, London, UK
    Crit Care Med 33:1903-12. 2005
    ..Here we investigate the effects of GSK-3beta inhibition on organ injury/dysfunction caused by lipopolysaccharide or coadministration of lipopolysaccharide and peptidoglycan in the rat...
  5. pmc Inhibition of gamma-secretase activity inhibits tumor progression in a mouse model of pancreatic ductal adenocarcinoma
    Ruben Plentz
    Department of Medicine, Massachusetts General Hospital Cancer Center, Harvard Medical School, Boston, Massachusetts 02114, USA
    Gastroenterology 136:1741-9.e6. 2009
    ..We investigated the role of this pathway in PDAC progression...
  6. pmc Inhibiting glycogen synthase kinase-3 reduces endotoxaemic acute renal failure by down-regulating inflammation and renal cell apoptosis
    Y Wang
    Department of Microbiology and Immunology, National Cheng Kung University Medical College, Tainan 701, Taiwan
    Br J Pharmacol 157:1004-13. 2009
    ..We investigated the effects of inhibiting GSK-3 on lipopolysaccharide (LPS)-induced acute renal failure, nuclear factor-kappaB (NF-kappaB), inflammation and apoptosis...
  7. doi 5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone
    Inga Cikotiene
    Laboratory of Biothermodynamics and Drug Design, Insitute of Biotechnology, Graiciuno 8, Vilnius LT 02241, Lithuania
    Bioorg Med Chem Lett 19:1089-92. 2009
    A series of 5-aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles were synthesized and their binding to several constructs of human Hsp90 chaperone measured by isothermal titration calorimetry (ITC)...
  8. pmc Store-operated Ca(2+) entry (SOCE) contributes to normal skeletal muscle contractility in young but not in aged skeletal muscle
    Angela M Thornton
    Department of Physiology and Biophysics, Robert Wood Johnson Medical School, Piscataway, NJ 08854, USA
    Aging (Albany NY) 3:621-34. 2011
    ....
  9. ncbi Synthesis, fungicidal activity, and 3D-QSAR of pyridazinone-substituted 1,3,4-oxadiazoles and 1,3,4-thiadiazoles
    Xia Juan Zou
    State Key Laboratory for Structural Chemistry Studies of Stable and Unstable Species, Institute of Physical Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing, P R China, 100871
    J Agric Food Chem 50:3757-60. 2002
    ..studied the structure and activity relationship of the compounds containing both pyridazinone-substituted 1,3,4-thiadiazoles and pyridazinone-substituted 1,3,4-oxadiazoles...
  10. ncbi Glycogen synthase kinase-3beta inhibitors protect against the organ injury and dysfunction caused by hemorrhage and resuscitation
    Laura Dugo
    Centre of Experimental Medicine, Nephrology and Critical Care, The William Harvey Research Institute, St Bartholomew s and the Royal London School of Medicine and Dentistry, Charterhouse Square, London EC1M 6BQ, UK
    Shock 25:485-91. 2006
    ..Thus, we propose that inhibition of GSK-3beta may represent a novel therapeutic approach in the therapy of hemorrhagic shock...
  11. ncbi Studies on synthesis and pharmacological activities of 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and their dihydro analogues
    Vinod Mathew
    Acharya and B M Reddy College of Pharmacy, Pharmaceutical Chemistry, 90 Soladevanahally, Hesaraghatta Road, Chikbanavara Post, Bangalore 560090, Karnataka, India
    Eur J Med Chem 42:823-40. 2007
    ..Synthesized compounds are studied for their antibacterial, antifungal, anti-inflammatory and analgesic activities. Some of the tested compounds showed significant pharmacological activities...
  12. doi Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles
    V Padmavathi
    Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India
    Eur J Med Chem 44:2106-12. 2009
    ..Interconversion of oxadiazoles to thiadiazoles and triazoles was carried out with appropriate reagents...
  13. doi Synthesis and in-vitro anticancer activity of 3,5-bis(indolyl)-1,2,4-thiadiazoles
    Dalip Kumar
    Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India
    Bioorg Med Chem Lett 21:5897-900. 2011
    A series of 3,5-bis(indolyl)-1,2,4-thiadiazoles were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines...
  14. doi Synthesis and antileishmanial activity of novel 5-(5-nitrofuran-2-y1)-1,3,4-thiadiazoles with piperazinyl-linked benzamidine substituents
    Azar Tahghighi
    Department of Medicinal Chemistry, School of Pharmacy and Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran
    Eur J Med Chem 46:2602-8. 2011
    In order to optimize the antileishmanial activity of piperazinyl-linked 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazoles, we synthesized a series of 5-(5-nitrofuran-2-y1)-1,3,4-thiadiazoles with piperazinyl-linked benzamidine substituent as ..
  15. ncbi Synthesis, antimicrobial and anti-inflammatory activities of some 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 1,2,4-triazolo[3,4-b][1,3,4]thiadiazines bearing trichlorophenyl moiety
    Prakash Karegoudar
    Sequent Scientific Limited, 120 A and B, Industrial Area, Bikampady, New Mangalore, Karnataka, India
    Eur J Med Chem 43:808-15. 2008
    ..All the synthesized compounds were screened for their antimicrobial and anti-inflammatory activities. Some of the compounds exhibited promising antimicrobial and anti-inflammatory activities...
  16. ncbi Synthesis and in vitro leishmanicidal activity of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles
    Alireza Foroumadi
    Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman 76351, Iran
    Bioorg Med Chem Lett 15:1983-5. 2005
    A series of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles (5a-d and 6a-j) were synthesized and evaluated against Leishmania major promastigotes using (3)H-thymidine incorporation...
  17. doi Synthesis of new chiral 2,5-disubstituted 1,3,4-thiadiazoles possessing gamma-butenolide moiety and preliminary evaluation of in vitro anticancer activity
    Meng Xue Wei
    Key Laboratory of Energy Sources and Chemical Engineering, Development Center of Natural Products and Medication and School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan, China
    Eur J Med Chem 44:3340-4. 2009
    A new series of chiral 1,3,4-thiadiazoles derivatives possessing gamma-substituted butenolide moiety were synthesized and evaluated for in vitro anticancer properties...
  18. ncbi Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies
    Fabrice Vergne
    Pfizer Global Research and Development, 3 9 Rue de la loge 94265 Fresnes, France
    Bioorg Med Chem Lett 14:4607-13. 2004
    ..The synthesis and SAR studies of a series of structurally novel small molecule inhibitors of PDE7 are discussed. The best compounds from the series displayed low nanomolar inhibitory activity and are selective versus PDE4...
  19. ncbi Evaluation of electronic, lipophilic and membrane affinity effects on antiproliferative activity of 5-substituted-2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles against various human cancer cells
    Joanna Matysiak
    Department of Chemistry, Agricultural University, Akademicka 15, 20 950 Lublin, Poland
    Eur J Med Chem 42:940-7. 2007
    The QSAR studies of 5-substituted-2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles set of antiproliferative activity against human cancer cell lines have been performed...
  20. doi Downregulation of Notch pathway by a gamma-secretase inhibitor attenuates AKT/mammalian target of rapamycin signaling and glucose uptake in an ERBB2 transgenic breast cancer model
    Clay L Efferson
    Department of Oncology, Pharmacology, Laboratory of Animal Research, Merck Research Laboratories, Boston, Massachusetts 02115, USA
    Cancer Res 70:2476-84. 2010
    ..These findings suggest that GSI may provide therapeutic benefit to a subset of ERBB2-positive breast cancers and that [(18)F]FDG-PET imaging may be useful in monitoring clinical response...
  21. ncbi 1-Acylthiosemicarbazides, 1,2,4-triazole-5(4H)-thiones, 1,3,4-thiadiazoles and hydrazones containing 5-methyl-2-benzoxazolinones: synthesis, analgesic-anti-inflammatory and antimicrobial activities
    Umut Salgın-Gökşen
    Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06100 Sihhiye, Ankara, Turkey
    Bioorg Med Chem 15:5738-51. 2007
    ..While most compounds were exhibiting high activity in the analgesic-anti-inflammatory field, most of them were found to be inactive against bacteria and fungi...
  22. doi Synthesis and anticancer activity of 5-(3-indolyl)-1,3,4-thiadiazoles
    Dalip Kumar
    Chemistry Group, Birla Institute of Technology and Science, Pilani, Rajasthan 333 031, India
    Eur J Med Chem 45:4664-8. 2010
    A series of 5-(3-indolyl)-2-substituted-1,3,4-thiadiazoles 5a-m were synthesized and their cytotoxicity analyzed against six human cancer cell lines...
  23. doi 5-Imino-1,2-4-thiadiazoles and quinazolines derivatives as glycogen synthase kinase 3β (GSK-3β) and phosphodiesterase 7 (PDE7) inhibitors: determination of blood-brain barrier penetration and binding to human serum albumin
    Daniel I Perez
    Instituto de Quimica Medica CSIC, Juan de Cierva 3, 28006 Madrid, Spain
    Eur J Pharm Sci 45:677-84. 2012
    5-Imino-1,2,4-thiadiazoles and quinazolines derivatives as glycogen synthase kinase 3β (GSK-3β) and phosphodiesterase 7 (PDE7) inhibitors were characterized for their ability to pass the blood-brain barrier (BBB) together with their ..
  24. ncbi Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles
    Zareen Amtul
    International Center for Chemical Sciences, HEJ Research Institute of Chemistry, University of Karachi, Karachi 75270, Pakistan
    Biochem Biophys Res Commun 319:1053-63. 2004
    ..Because of their safe profile in the genotoxic assay, they may be pursued in the near future for human testing..
  25. doi Glycogen synthase kinase 3 inhibition protects the heart from acute ischemia-reperfusion injury via inhibition of inflammation and apoptosis
    Hao Kao Gao
    Department of Cardiology, Xi Jing Hospital, Fourth Military Medical University Xi an, China
    J Cardiovasc Pharmacol 52:286-92. 2008
    ..22 +/- 2%, P < 0.05). Therefore, blocking this protein kinase activity may be a novel approach to the treatment of this condition, which is characterized by inflammation and apoptosis...
  26. doi Synthesis of 3-((2,4-dichlorophenoxy)methyl)-1,2,4-triazolo(thiadiazoles and thiadiazines) as anti-inflammatory and molluscicidal agents
    M F El Shehry
    National Research Centre, Green Chemistry Department, 12622 Dokki, Cairo, Egypt
    Eur J Med Chem 45:1906-11. 2010
    ..The compounds 4b, 4d, 11 and 14 showed potent anti-inflammatory activities in dose dependent manner while compounds 3, 4b, 8 and 10 exhibited promising molluscicidal activities...
  27. ncbi Synthesis and antiviral activity evaluation of some new 6-substituted 3-(1-adamantyl)-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles
    Marina Kritsanida
    Department of Pharmacy, University of Athens, Greece
    Farmaco 57:253-7. 2002
    ..No antiviral effects were noted with any of the compounds at subtoxic concentrations in cell culture...
  28. ncbi Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action
    Anikó Göblyös
    Leiden Amsterdam Center for Drug Research, Division of Medicinal Chemistry, P O Box 9502, 2300 RA Leiden, The Netherlands
    J Med Chem 48:1145-51. 2005
    ..We suggest that the thiadiazoles are sulfhydryl modifying agents rather than allosteric modulators, as they appear to reversibly modify the ..
  29. ncbi Ca2+-independent phospholipase A2 enhances store-operated Ca2+ entry in dystrophic skeletal muscle fibers
    François Xavier Boittin
    Laboratory of Pharmacology, Geneva Lausanne School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, 1211 Geneva 4, Switzerland
    J Cell Sci 119:3733-42. 2006
    ..The Ca2+-independent phospholipase A2 pathway therefore appears as an attractive target to reduce excessive Ca2+ influx and subsequent degeneration occurring in dystrophic fibers...
  30. doi Synthesis, characterization, and in vitro antimicrobial activities of 5-alkenyl/hydroxyalkenyl-2-phenylamine-1,3,4-oxadiazoles and thiadiazoles
    Nida N Farshori
    Department of Chemistry, Aligarh Muslim University, Aligarh, India
    Bioorg Med Chem Lett 20:1933-8. 2010
    ..4a-d), which on further refluxing with POCl(3) and Ac(2)O yielded corresponding 1,3,4-oxadiazoles (3a-d) and thiadiazoles (5a-d), respectively...
  31. ncbi Synthesis and anti-inflammatory activity of 1-acylthiosemicarbazides, 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazole-3-thiones
    Erhan Palaska
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey
    Farmaco 57:101-7. 2002
    ..Side effects of the compounds were examined on gastric mucosa, liver and stomach and none of the compounds showed significant side effects compared with reference nonsteroidal anti-inflammatory drugs (NSAIDs)...
  32. pmc Inhibition of glycogen synthase kinase-3beta attenuates the development of carrageenan-induced lung injury in mice
    S Cuzzocrea
    Department of Clinical and Experimental Medicine and Pharmacology, School of Medicine, University of Messina, Messina, Italy
    Br J Pharmacol 149:687-702. 2006
    ..Here, we have investigated the effects of TDZD-8, a potent and selective GSK-3beta inhibitor, in a mouse model of carrageenan-induced pleurisy...
  33. ncbi First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease
    Ana Martinez
    Instituto de Quimica Medica CSIC, Juan de la Cierva 3, 28006 Madrid, Spain
    J Med Chem 45:1292-9. 2002
    ..SAR studies allowed the identification of the key structural features. Finally, a possible enzymatic binding mode is proposed...
  34. ncbi Glycogen synthase kinase-3 beta inhibition reduces secondary damage in experimental spinal cord trauma
    Salvatore Cuzzocrea
    Department of Clinical and Experimental Medicine and Pharmacology, School of Medicine, University of Messina, Torre Biologica, Policlinico Universitario Via C Valeria, Gazzi 98100 Messina Italy
    J Pharmacol Exp Ther 318:79-89. 2006
    ..Taken together, our results clearly demonstrate that treatment with TDZD-8 reduces the development of inflammation and tissue injury associated with spinal cord trauma...
  35. ncbi Differences in kinetics of xanomeline binding and selectivity of activation of G proteins at M(1) and M(2) muscarinic acetylcholine receptors
    Jan Jakubik
    Department of Neurochemistry, Institute of Physiology CAS, Videnska 1083, 14220 Prague, Czech Republic
    Mol Pharmacol 70:656-66. 2006
    ..These conformations are both time- and concentration-dependent and vary between the M(1) and the M(2) receptor...
  36. pmc Rapid and selective death of leukemia stem and progenitor cells induced by the compound 4-benzyl, 2-methyl, 1,2,4-thiadiazolidine, 3,5 dione (TDZD-8)
    Monica L Guzman
    James P Wilmot Cancer Center, University of Rochester, NY 14642, USA
    Blood 110:4436-44. 2007
    ..We conclude that TDZD-8 uses a unique and previously unknown mechanism to rapidly target leukemia cells, including malignant stem and progenitor populations...
  37. ncbi Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia
    Anantha Shekhar
    Department of Psychiatry, Indiana University School of Medicine, 1111 West 10th St, Suite 313, Indianapolis, IN 46202, USA
    Am J Psychiatry 165:1033-9. 2008
    ..The authors studied xanomeline, a relatively selective muscarinic type 1 and type 4 (M(1) and M(4)) receptor agonist, to determine if this agent is effective in the treatment of schizophrenia...
  38. pmc Growth control of multiple myeloma cells through inhibition of glycogen synthase kinase-3
    Ying Zhou
    Department of Medicine, University of Chicago, Chicago, IL 60637, USA
    Leuk Lymphoma 49:1945-53. 2008
    ..The levels of the pro-apoptotic proteins Fas ligand (FasL) and IkappaBalpha increased after treatment with TDZD in myeloma cell lines. These studies provide the basis for further testing of GSK3 inhibitors in the clinical setting...
  39. ncbi Allosteric modulation by persistent binding of xanomeline of the interaction of competitive ligands with the M1 muscarinic acetylcholine receptor
    Jan Jakubik
    Institute of Physiology, Academy of Sciences of the Czech Republic, Prague, Czech Republic
    J Pharmacol Exp Ther 301:1033-41. 2002
    ..Our findings are best interpreted in terms of allosteric interactions between xanomeline-persistent binding to the M(1) muscarinic receptor and competitive ligands bound to the classical receptor binding site...
  40. ncbi Activation of p53-dependent apoptosis by acute ablation of glycogen synthase kinase-3beta in colorectal cancer cells
    Jagadish C Ghosh
    Department of Cancer Biology and Cancer Center, University of Massachusetts Medical School, Worcester, Massachusetts 01605, USA
    Clin Cancer Res 11:4580-8. 2005
    ..A pivotal signaling network in colorectal cancer cells involves glycogen synthase kinase-3beta (GSK3beta), a multifunctional kinase whose role in tumor cell survival is not defined...
  41. pmc Reduction of experimental colitis in the rat by inhibitors of glycogen synthase kinase-3beta
    Brendan J R Whittle
    Centre for Experimental Therapeutics, William Harvey Research Institute, Barts and The London, Queen Mary s School of Medicine and Dentistry, Charterhouse Square, London, EC1M 6BQ, UK
    Br J Pharmacol 147:575-82. 2006
    ..The mechanisms underlying this anti-inflammatory action may be related to downregulation of NF-kappaB activity, involved in the generation of proinflammatory mediators...
  42. ncbi Insulin reduces the multiple organ injury and dysfunction caused by coadministration of lipopolysaccharide and peptidoglycan independently of blood glucose: role of glycogen synthase kinase-3beta inhibition
    Laura Dugo
    Centre for Experimental Medicine, Nephrology and Critical Care Medicine, The William Harvey Research Institute, St Bartholomew s and the Royal London School of Medicine and Dentistry, Charterhouse Square, London, UK
    Crit Care Med 34:1489-96. 2006
    ..Here we investigate the role of blood glucose and glycogen synthase kinase-3beta inhibition in the protective effect of insulin on the organ injury/dysfunction associated with excessive systemic inflammation...
  43. ncbi Glycogen synthase kinase-3beta inhibition attenuates the degree of arthritis caused by type II collagen in the mouse
    Salvatore Cuzzocrea
    Institute of Pharmacology, School of Medicine, University of Messina, Torre Biologica Policlinico Universitario, Via C Valeria Gazzi 98100 Messina, Italy
    Clin Immunol 120:57-67. 2006
    ..These data demonstrate that GSK-3beta inhibition exerts an anti-inflammatory effect during chronic inflammation and is able to ameliorate the tissue damage associated with CIA...
  44. ncbi Heterocyclic system containing bridgehead nitrogen atom: synthesis and pharmacological activities of some substituted 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles
    V Mathew
    Acharya and B M Reddy College of Pharmacy, Bangalore, Karnataka, India
    Eur J Med Chem 41:1048-58. 2006
    ..Synthesized triazolo thiadiazoles investigated for their antibacterial, antifungal, anti-inflammatory and analgesic activities...
  45. ncbi Inhibition of GSK-3beta mediates expression of MMP-9 through ERK1/2 activation and translocation of NF-kappaB in rat primary astrocyte
    Sun Don Kim
    Laboratory of Pharmacology, College of Pharmacy, Seoul National University, Seoul 151 742, Republic of Korea
    Brain Res 1186:12-20. 2007
    ..These data suggest that GSK-3beta inhibition mediates ERK1/2 activation followed by NF-kappaB activation, which directly regulates the induction of MMP-9 in rat primary astrocytes...
  46. pmc Long-term wash-resistant effects of brief interaction of xanomeline at the M1 muscarinic receptor
    Kayla C De Lorme
    Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Mayo Mail Code 392, 420 Delaware St SE, Minneapolis, MN 55455, USA
    Neurosci Lett 410:11-4. 2006
    ..However, possible involvement of other mechanisms of long-term receptor regulation cannot be discounted...
  47. ncbi Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors
    Adrianus M C H van den Nieuwendijk
    Leiden Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Leiden University, P O Box 9502, 2300RA Leiden, The Netherlands
    J Med Chem 47:663-72. 2004
    ..Compounds 7a and 7l displayed peculiar displacement characteristics of both radiolabeled agonist and antagonist binding to A(2A) receptors, whereas 7a showed some activity on A(3) receptors...
  48. ncbi Role of receptor protein and membrane lipids in xanomeline wash-resistant binding to muscarinic M1 receptors
    Jan Jakubik
    Institute of Physiology, Academy of Sciences of the Czech Republic, Prague
    J Pharmacol Exp Ther 308:105-10. 2004
    ..We suggest that the binding of xanomeline involves interhelical penetration of M1 muscarinic receptor by xanomeline's O-alkyl chain and interaction with membrane lipids surrounding the receptor...
  49. ncbi Xanomeline compared to other muscarinic agents on stimulation of phosphoinositide hydrolysis in vivo and other cholinomimetic effects
    F P Bymaster
    Lilly Neuroscience Research, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Brain Res 795:179-90. 1998
    ....
  50. ncbi On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor
    A Christopoulos
    Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Minneapolis, Minnesota 55455, USA
    Mol Pharmacol 53:1120-30. 1998
    ....
  51. doi Synthesis, antioxidant properties and radioprotective effects of new benzothiazoles and thiadiazoles
    Damien Cressier
    Laboratoire Hétérochimie Fondamentale et Appliquée, UMR 5069 CNRS UPS, Universite Paul Sabatier, 118, route de Narbonne, 31062 Toulouse Cedex 9, France
    Bioorg Med Chem 17:5275-84. 2009
    In this work, we report the synthesis and characterization of new compounds derived from benzothiazoles and thiadiazoles. We observed that structural modifications on these skeletons affected the antioxidant activity...
  52. ncbi Long-term changes in the muscarinic M1 receptor induced by instantaneous formation of wash-resistant xanomeline-receptor complex
    Kayla C De Lorme
    Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Minneapolis, MN 55455, USA
    J Pharmacol Exp Ther 323:868-76. 2007
    ..Our results imply that brief exposure to xanomeline followed by washing and prolonged waiting may result in delayed receptor desensitization accompanied by internalization or down-regulation...
  53. doi Facile synthesis of substituted 5-amino- and 3-amino-1,2,4-thiadiazoles from a common precursor
    Paul M Wehn
    Department of Medicinal Chemistry, Amgen Inc, 1120 Veterans Boulevard, South San Francisco, California 94080, USA
    Org Lett 11:5666-9. 2009
    A novel approach to the synthesis of substituted 5-amino- and 3-amino-1,2,4-thiadiazoles beginning from a common precursor has been achieved...
  54. pmc Insulin reduces cerebral ischemia/reperfusion injury in the hippocampus of diabetic rats: a role for glycogen synthase kinase-3beta
    Massimo Collino
    Department of Anatomy, Pharmacology, and Forensic Medicine, University of Turin, Turin, Italy
    Diabetes 58:235-42. 2009
    ..Insulin is a well-known inhibitor of glycogen synthase kinase-3beta (GSK-3beta). Here, we investigate the role of GSK-3beta inhibition on I/R-induced cerebral injury in a rat model of insulinopenic diabetes...
  55. pmc Benzothiadiazole, a novel class of inducers of systemic acquired resistance, activates gene expression and disease resistance in wheat
    J Gorlach
    Ciba Geigy Agricultural Biotechnology Research Unit, Research Triangle Park, North Carolina 27709 2257, USA
    Plant Cell 8:629-43. 1996
    ..BTH is being developed commercially as a novel type of plant protection compound that works by inducing the plant's inherent disease resistance mechanisms...
  56. ncbi Effect of a new 1,3,4-thiadiazolium mesoionic compound (MI-D) on B16-F10 murine melanoma
    Andrea Senff-Ribeiro
    Departments of Biochemistry and Cellular Biology, Federal University of Parana, Curitiba, Parana, Brazil
    Melanoma Res 13:465-71. 2003
    ..On day 17, tumours were excised and their weights were determined. MI-D inhibited tumour growth by 85%. This is a very encouraging result with regard to the possibility of MI-D becoming a new tool for melanoma research and treatment...
  57. ncbi Interference of MI-D, a new mesoionic compound, on artificial and native membranes
    Silvia M S C Cadena
    Departamento de Bioquimica, Universidade Federal do Parana, Curitiba, Brasil
    Cell Biochem Funct 20:31-7. 2002
    ..These alterations in membrane fluidity are thus related to MI-D effects on the energy-linked functions of mitochondria...
  58. ncbi Novel persistent activation of muscarinic M1 receptors by xanomeline
    A Christopoulos
    Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Minneapolis 55455, USA
    Eur J Pharmacol 334:R3-4. 1997
    ..This phenomenon was not observed with carbachol. This is the first report of a persistent, receptor-activating effect of a muscarinic agonist...
  59. ncbi Synthesis and antiproliferative activity of some 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles
    Joanna Matysiak
    Department of Chemistry, Agricultural University, Lublin, Poland
    Eur J Med Chem 41:475-82. 2006
    A series of new 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles has been synthesised and evaluated for their antiproliferative activity...
  60. ncbi NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders
    Rosario Luna-Medina
    Instituto de Investigaciones Biomedicas, Consejo Superior de Investigaciones Cientificas, Universidad Autonoma de Madrid, 28029 Madrid, Spain
    J Neurosci 27:5766-76. 2007
    ..As such, these findings identify NP031112 as a potential therapeutic agent for the treatment of neurodegenerative disorders...
  61. ncbi Antimelanoma activity of 1,3,4-thiadiazolium mesoionics: a structure-activity relationship study
    Andrea Senff-Ribeiro
    Department of Biochemistry, Federal University of Parana, Curitiba, PR, Brazil
    Anticancer Drugs 15:269-75. 2004
    ..This seems to be important for degree of anti-tumor activity of these compounds...
  62. ncbi Treatment with the glycogen synthase kinase-3beta inhibitor, TDZD-8, affects transient cerebral ischemia/reperfusion injury in the rat hippocampus
    Massimo Collino
    Department of Anatomy, Pharmacology and Forensic Medicine, University of Turin, Turin, Italy
    Shock 30:299-307. 2008
    ..The present study demonstrates that TDZD-8 protects the brain against I/R injury by inhibiting GSK-3beta activity. Collectively, our data may contribute to focus the role of GSK-3beta in cerebral I/R...
  63. ncbi Environmentally sensitive, SA-dependent defense responses in the cpr22 mutant of Arabidopsis
    K Yoshioka
    Boyce Thompson Institute for Plant Research, Tower Road, Ithaca, NY 14853, USA
    Plant J 26:447-59. 2001
    ..Interestingly, the SA-dependent phenotypes, but not the SA-independent phenotypes, are suppressed when cpr22 mutants are grown under high humidity...
  64. ncbi The influence of growth regulators on shoot proliferation and rooting of in vitro propagated caper
    G Caglar
    Department of Horticulture, Faculty of Agriculture, Kahramanmaras Sutcu Imam University, Turkey
    J Environ Biol 26:479-85. 2005
    ..Dipping the caper shoots in the solution of IBA at 24.6 microM for 10 minutes before planting on MS media, improved the rooting percentage up to 80.5% under a 16 hr photoperiod...
  65. ncbi TDZ, auxin and genotype effects on leaf organogenesis in Fragaria
    L Landi
    Dipartimento di Scienze Ambientali e delle Produzioni Vegetali, Marche Polytechnic University, Via Brecce Bianche, 60100 Ancona, Italy
    Plant Cell Rep 25:281-8. 2006
    ..143.5). For the more efficient regenerating genotypes, IBA induced the highest frequency of regenerating leaves, while BSAA induced the highest number of regenerated shoots from leaves and more callus production for most of the genotypes...
  66. ncbi [A protector effect of cytokinin preparations on the photosynthetic apparatus of wheat plants under water deficiency conditions]
    O F Monakhova
    Prikl Biokhim Mikrobiol 43:720-9. 2007
    ..The negative influence of water stress on the photosynthetic apparatus was more pronounced in a less tolerant cultivar Lutescens 758 and in the seedlings as compared with the adult plants...
  67. ncbi In vitro plant regeneration from leaf-derived callus of Cimicifuga racemosa
    Hemant Lata
    National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, The University of Mississippi, University, 38677, USA
    Planta Med 68:912-5. 2002
    ..Activated charcoal was an essential component for vigorous rooting formation. Our results suggest that conservation of C. racemosa is possible through in vitro multiplication of leaf-derived callus...
  68. pmc Transgenic studies on the involvement of cytokinin and gibberellin in male development
    Shihshieh Huang
    Mystic Research, Monsanto Company, St Louis, Missouri 63198, USA
    Plant Physiol 131:1270-82. 2003
    ....
  69. ncbi Synthesis and antioxidant properties of novel N-methyl-1,3,4-thiadiazol-2-amine and 4-methyl-2H-1,2,4-triazole-3(4H)-thione derivatives of benzimidazole class
    Canan Kus
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Ankara, Turkey
    Bioorg Med Chem 16:4294-303. 2008
    ..Compound 17c inhibited the microsomal ethoxyresorufin O-deethylase (EROD) activity with an IC(50)=4.5 x 10(-4)M which is similarly better than the specific inhibitor caffeine IC(50)=5.2 x 10(-4)M...
  70. ncbi Correlation of epiphyllous bud differentiation with foliar senescence in crassulacean succulent Kalanchoe pinnata as revealed by thidiazuron and ethrel application
    Sarita Jaiswal
    Plant Physiology Laboratory, Department of Botany, University of Delhi, Delhi 110 007, India
    J Plant Physiol 163:717-22. 2006
    ..A working hypothesis to interpret responsiveness of the disc-bud composite on lines of a source-sink duo, has been proposed...
  71. ncbi Involvement of phospholipases C and D in early response to SAR and ISR inducers in Brassica napus plants
    B Profotova
    Department of Biochemistry and Microbiology, Institute of Chemical Technology Prague, Technicka 3, 166 28 Prague 6, Czech Republic
    Plant Physiol Biochem 44:143-51. 2006
    ..These results show that phospholipases are involved in very early processes leading to systemic responses in plants and that they are most probably initially first activated on post translational level...
  72. ncbi Hormone-regulated inflorescence induction and TFL1 expression in Arabidopsis callus in vitro
    C M Guan
    Shandong Key Laboratory of Crop Biology, College of Life Sciences, Shandong Agricultural University, Taian, Shandong, 271018, China
    Plant Cell Rep 25:1133-7. 2006
    ..Furthermore, TFL1, a gene involved in floral transition in Arabidopsis, was activated during the inflorescence induction. Our results suggest that the TFL1 gene plays an important role in hormone-regulated inflorescence formation...
  73. ncbi Regeneration of the Egyptian medicinal plant Artemisia judaica L
    C Z Liu
    Department of Plant Agriculture, Biotechnology Division, Edmund C Bovey Complex, University of Guelph, N1G 2W1 Guelph, Ontario, Canada
    Plant Cell Rep 21:525-30. 2003
    ..The regeneration protocol developed in this study provides a basis for germplasm conservation and for further investigation of medicinally active constituents of A. judaica...
  74. ncbi beta-Aminobutyric acid-induced resistance against downy mildew in grapevine acts through the potentiation of callose formation and jasmonic acid signaling
    Mollah Md Hamiduzzaman
    University of Neuchatel, Institute of Botany, Department of Biochemistry, Rue Emile Argand 11, Case Postale 2, CH 2007 Neuchatel, Switzerland
    Mol Plant Microbe Interact 18:819-29. 2005
    ....
  75. ncbi Optimizing regeneration condition in chickpea (Cicer arietinum L.)
    Mahdieh Yousefiara
    Department of Biotechnology and Plant Breeding, Faculty of Agriculture, Ferdowsi University of Mashhad, P O Box 91775 1163, Mashhad, Iran
    Pak J Biol Sci 11:1009-14. 2008
    ..4 mg L(-1) IBA) for 7 to 14 days, then transferred to pots filled by cocopit: perlite (1:1) and kept in a growth chamber until their shoots and roots were well developed. This resulted in more than 70% survival rate...
  76. ncbi A highly efficient plant regeneration system through multiple shoot differentiation from commercial cultivars of barley (Hordeum vulgare L.) using meristematic shoot segments excised from germinated mature embryos
    Vijendra K Sharma
    Department of Plant Biology, Technical University of Braunschweig, Humboldtstr 1, 38106, Braunschweig, Germany
    Plant Cell Rep 23:9-16. 2004
    ..All of the genotypes tested formed multiple shoots. The percentage of relative MSS multiplication was 63-83%, and the average number of multiplied shoots per MSS ranged from 16 to 34 among the genotypes after 9-11 weeks...
  77. ncbi Transgene expression in strawberries driven by a heterologous phloem-specific promoter
    Yan Zhao
    Molecular Plant Pathology Laboratory, USDA Agriculture Research Service, Beltsville, MD 20705, USA
    Plant Cell Rep 23:224-30. 2004
    ..The results suggest that the transformation protocol and the AtSUC2 promoter may be useful for engineering phytoplasma-resistant transgenic strawberries...
  78. ncbi In vitro regeneration of Salix nigra from adventitious shoots
    Satu Lyyra
    Daniel B Warnell School of Forest Resources, University of Georgia, Athens, GA 30602, USA
    Tree Physiol 26:969-75. 2006
    ..The ability of black willow inflorescences to produce adventitious shoots makes them potential targets for Agrobacterium-mediated transformation with heavy-metal-resistant genes for phytoremediation...
  79. ncbi Synthesis and anti-inflammatory evaluation of methylene bridged benzofuranyl imidazo[2,1-b][1,3,4]thiadiazoles
    V B Jadhav
    Department of Chemistry, Karnatak University, Dharwad 580 003, Karnataka, India
    Eur J Med Chem 43:1721-9. 2008
    A series of 6-substituted and 5,6-disubstituted 2-(6-methyl-benzofuran-3-ylmethyl)-imidazo[2,1-b][1,3,4]thiadiazoles have been synthesized. The new compounds have been tested for their in vivo analgesic, anti-inflammatory activities...
  80. ncbi Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators
    Mark C Manfredi
    Bristol Myers Squibb Research and Development, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 17:4487-90. 2007
    ..Replacement of the 3-oxo group of 2-chloro-4-[(7R,7aS)-7-hydroxy-1,3-dioxotetrahydro-1H-pyrrolo[1,2c]imidazol-2(3H)-yl]-3-methylbenzonitrile resulted in a sulfamide series of selective androgen receptor modulator (SARM) agonists...
  81. ncbi An efficient adventitious shoot regeneration system for Zhanhua winter jujube (Zizyphus jujuba Mill.) using leaf explants
    X F Gu
    School of Life Science, Shandong University, 27 Shanda Nanlu, Jinan, 250100, P R China
    Plant Cell Rep 23:775-9. 2005
    ..14 microM IAA and 2.46 microM indolebutyric acid to induce rooting. This system of adventitious shoot production from leaf explants of adult plants could be useful for the genetic engineering and polyploidization of winter jujube...
  82. ncbi High-frequency shoot multiplication in Curcuma longa L using thidiazuron
    S Prathanturarug
    Department of Pharmaceutical Botany, Faculty of Pharmacy, Mahidol University, 447 Sri Ayudthaya Road, 10400, Bangkok, Thailand
    Plant Cell Rep 21:1054-9. 2003
    ..22+/-0.62 shoots/explant was obtained after 12 weeks of cultures. Spontaneous rooting was achieved. The regenerated plants were transferred to soil under greenhouse conditions and subsequently grown successfully in the field...
  83. ncbi In vitro regeneration of Hagenia abyssinica (Bruce) J.F. Gmel. (Rosaceae) from leaf explants
    T Feyissa
    Department of Crop Science, Swedish University of Agricultural Sciences, P O Box 44, 230 53 Alnarp, Sweden
    Plant Cell Rep 24:392-400. 2005
    ..A significant (P< or =0.05) difference in regeneration capacity was observed among the five genotypes examined. The resulting shoots were multiplied on multiplication medium, rooted and acclimatised in a greenhouse...
  84. ncbi Artemisinin production by shoot regeneration of Artemisia annua L. using thidiazuron
    Wanwimon Lualon
    Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, 40002, Thailand
    Z Naturforsch C 63:96-100. 2008
    ..73 -/+ 0.23) microg/mg DW]. This system exhibited a potential for a rapid propagation of shoots from the stem explant and makes it possible to develop a clonal propagation of A. annua...
  85. ncbi Thidiazuron induces shoot organogenesis at low concentrations and somatic embryogenesis at high concentrations on leaf and petiole explants of African violet (Saintpaulia ionantha Wendl)
    J Mithila
    Department of Environmental Biology, University of Guelph, Ontario, Canada N1G 2W1
    Plant Cell Rep 21:408-14. 2003
    ..These findings provide the first report of simultaneous shoot organogenesis and somatic embryogenesis of African violet explants in response to TDZ...
  86. ncbi Direct somatic embryogenesis and synthetic seed production from Paulownia elongata
    Z Ipekci
    TUBITAK, Research Institute for Genetic Engineering and Biotechnology, P O Box 21, 41470 Gebze Kocaeli, Turkey
    Plant Cell Rep 22:16-24. 2003
    ..8% and 53.5% and the germination frequencies were 43.2% and 32.4%, respectively. These systems could be useful for the rapid clonal propagation and dissemination of synthetic seed material of Paulownia elongata...
  87. ncbi In vitro micropropagation of Boswellia ovalifoliolata
    Thummala Chandrasekhar
    Department of Botany, Sri Venkateswara Univerity, AP, India
    Z Naturforsch C 60:505-7. 2005
    ..Activated charcoal (100 mg l(-1)) and polyvinylpyrrolidone (40 mg l(-1)) were added to the medium to prevent browning of cultures. The regenerated plantlets have been successfully acclimatized and transferred to soil...
  88. ncbi Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations
    Danzhi Huang
    Department of Biochemistry, University of Zurich, Winterthurerstrasse 190, CH 8057 Zurich, Switzerland
    J Med Chem 48:5108-11. 2005
    ..In particular, the phenylureathiadiazole 2 and the diphenylurea derivative 3 are promising lead compounds for beta-secretase inhibition...
  89. ncbi Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-thiadiazole- and 1,2,4-triazole-thiols
    Gabriela Laura Almajan
    Organic Chemistry Department, Faculty of Pharmacy, Traian Vuia Street 6, 77210 Bucharest, Romania
    Bioorg Med Chem Lett 15:2347-52. 2005
    ..9-618 microM, and against hCA IX in the range of 9.3-772 microM. Thiadiazoles were generally more active than triazoles against all investigated isozymes...
  90. ncbi Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors
    Robert M Rzasa
    Department of Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, CA 91320 1789, USA
    Bioorg Med Chem 15:6574-95. 2007
    ..In this investigation we present our synthetic studies toward this series of compounds and discuss their biological relevance as CDK5 inhibitors...
  91. ncbi Design, synthesis, and docking studies of new 1,3,4-thiadiazole-2-thione derivatives with carbonic anhydrase inhibitory activity
    Mohammed K Abdel-Hamid
    Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
    Bioorg Med Chem 15:6975-84. 2007
    ..The results showed similar orientation of the target compounds at CA II active site compared with reported sulfonamide type CAIs with the thione group acting as a zinc-binding moiety...
  92. ncbi Synthesis and anticancer activity of a novel class of flavonoids: 2,4-diarylchromane[4,3-d]-delta(1,9b)-1,2,3-thiadiazolines
    Huazhou Ying
    ZJU ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, China
    Eur J Med Chem 42:226-34. 2007
    ..Mechanism research indicated that it is due to 11a that induces DNA fragmentation...
  93. doi Novel aminopeptidase N inhibitors derived from 1,3,4-thiadiazole scaffold
    GuoGang Tu
    Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Ji nan 250012, PR China
    Bioorg Med Chem 16:6663-8. 2008
    ..In this study, we report the synthesis and in vitro enzyme inhibition assay of 1,3,4-thiadiazole scaffold compounds. These new compounds have potent inhibitory activities toward APN with IC(50) values in the micromol rang...
  94. ncbi A chemometric study of megazol derivatives with activity against Trypanosoma equiperdum
    F P Rosselli
    Departamento de Quimica e Fisica Molecular, Instituto de Quimica de Sao Carlos, Universidade de Sao Paulo, CP 780, 13560 970 Sao Carlos SP, Brazil
    SAR QSAR Environ Res 17:533-47. 2006
    ..equiperdum...
  95. ncbi [Synthesis and antibacterial activity of 3-(4-piperazin-1-yl-phenyl)-s-triazolo [3,4-b] [1,3,4] thiadiazole hydrochlorides]
    Guo Qiang Hu
    Institute of Pharmacy, Henan University, Kaifeng 475004, China
    Yao Xue Xue Bao 42:54-7. 2007
    ..group, the nucleophilic substitution of 3-(4-chlorophenyl)-6-substituted-s-triazolo-[3, 4-b] [1, 3, 4] thiadiazoles (2a - n) with piperazine in the presence of phase transfer catalyst TBAI afforded 3-(4-piperazin-1-yl-phenyl)-6-..
  96. ncbi Studies toward the structural optimization of new brazilizone-related trypanocidal 1,3,4-thiadiazole-2-arylhydrazone derivatives
    Samir A Carvalho
    Fundacao Oswaldo Cruz, Instituto de Tecnologia em Fármacos Far Manguinhos, Laboratório de Síntese IV, 21041 250 Rio de Janeiro, RJ, Brazil
    Bioorg Med Chem 16:413-21. 2008
    ..Herein we report the synthesis and trypanocidal profile of thirteen new Brazilizone A analogues, which supported the construction of 3D-QSAR models used for its structural optimization...
  97. ncbi Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor
    Brian E Kane
    Department of Medicinal Chemistry, Center for Drug Design, University of Minnesota, Minneapolis, MN 55455, USA
    Bioorg Med Chem 16:1376-92. 2008
    ..Herein, a qualitative model that accounts for both binding scenarios is proposed and applied to understand the structural basis to wash-resistant binding and long-acting effects of xanomeline-based compounds...
  98. ncbi Synthesis and evaluation of antitubercular activity of imidazo[2,1-b][1,3,4]thiadiazole derivatives
    Gundurao Kolavi
    Department of Chemistry, Karnatak University, Dharwad, India
    Bioorg Med Chem 14:3069-80. 2006
    A series of 2,6-disubstituted and 2,5,6-trisubstituted imidazo[2,1-b][1,3,4]thiadiazoles were synthesized, the structures of the compounds were elucidated and screened for antitubercular activity against Mycobacterium tuberculosis H37Rv ..
  99. ncbi Synthesis and antitrypanosomal profile of new functionalized 1,3,4-thiadiazole-2-arylhydrazone derivatives, designed as non-mutagenic megazol analogues
    Samir A Carvalho
    Instituto de Quimica, Universidade Federal do Rio de Janeiro, 21949900 Rio de Janeiro, RJ, Brazil
    Bioorg Med Chem Lett 14:5967-70. 2004
    ..The evaluation of the activity against bloodstream trypomastigote forms of Trypanosoma cruzi forms lead us to identify a new potent trypamomicide prototype, that is, brazilizone A (4k), which present an IC50/24 h=5.3 microM...
  100. doi Synthesis and antifungal activity of novel sulfoxide derivatives containing trimethoxyphenyl substituted 1,3,4-thiadiazole and 1,3,4-oxadiazole moiety
    Fang Liu
    Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China
    Bioorg Med Chem 16:3632-40. 2008
    ..After treating with compound 10a at 100 microg/mL for 12 h, the mycelial reducing sugar, D-GlcNAc, soluble protein and pyruvate content, chitinase activity showed declining tendency...
  101. ncbi Synthesis and antibacterial activity of N-[5-(chlorobenzylthio)-1,3,4-thiadiazol-2-yl] piperazinyl quinolone derivatives
    Alireza Foroumadi
    Pharmaceutical Sciences Research Center Tehran University of Medical Sciences, Tehran, Iran
    Arch Pharm Res 30:138-45. 2007
    ..4a-I) have been synthesized by reaction of piperazinyl quinolones with 5-chloro-2-(chlorobenzylthio)-1,3,4-thiadiazoles. Their structures were confirmed by elemental analysis, IR and NMR spectra...

Research Grants87

  1. Serotonin and CRF Pathways in Anxiety & HPA Regulation
    Anantha Shekhar; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  2. METABOLISM AND ANTITUMOR ACTIVITY OF AMINOTHIADIAZOLES
    Donald Hill; Fiscal Year: 1980
    ..If such a system can not be obtained, NAD+ analogs containing thiadiazoles will be prepared utilizing NADase and then hydrolyzed with nucleotide pyrophosphatase to yield thiadiazole ..
  3. Novel HBV Therapeutic with Potential for Treatment of Drug-Resistant Infection
    Andrea Cuconati; Fiscal Year: 2008
    ..At the end of the proposed project, the novel compound would be ready for large-scale Phase III clinical testing with hepatitis B patients. [unreadable] [unreadable] [unreadable]..
  4. A mechanism for suppression of TNF induced endothelial dysfunction
    Arnold Johnson; Fiscal Year: 2010
    ..Thus, successful completion of the proposed studies may result in progress in treatment and prevention of advanced sepsis/ARDS. ..
  5. Muscarinic agonists for neurological disorders
    William Messer; Fiscal Year: 2006
    ..The studies outlined here will provide new approaches for the treatment of neurological disorders, including Alzheimer's disease and schizophrenia. ..
  6. Metal-Mediated Routes to Biaryls
    Bruce Lipshutz; Fiscal Year: 2006
    ..A particular, albeit representative, application of a novel substituted cyclo-NOBIN will be studied for selected asymmetric aldol reactions. ..
  7. A mechanism for TNF induced endothelial dysfunction
    Arnold Johnson; Fiscal Year: 2006
    ..abstract_text> ..
  8. Cellular and Molecular Studies of Leukemic Stem Cellss
    Craig Jordan; Fiscal Year: 2006
    ..Collectively, these efforts will advance our understanding of basic mechanisms that underlie leukemic transformation and will improve strategies for the preferential ablation of LSCs. ..
  9. Metal-Mediated Routes to Biaryls
    Bruce Lipshutz; Fiscal Year: 2005
    ..A particular, albeit representative, application of a novel substituted cyclo-NOBIN will be studied for selected asymmetric aldol reactions. ..
  10. NEUROLEPTIC SPACER LENGTH GOVERNS MOLECULAR RECOGNITION
    John Schetz; Fiscal Year: 2005
    ....
  11. Muscarinic agonists for neurological disorders
    William Messer; Fiscal Year: 2004
    ..The studies outlined here will provide new approaches for the treatment of neurological disorders, including Alzheimer's disease and schizophrenia. ..
  12. NEUROLEPTIC SPACER LENGTH GOVERNS MOLECULAR RECOGNITION
    John Schetz; Fiscal Year: 2004
    ....
  13. NATURALLY OCCURRING POLYENES VIA ORGANOMETALLICS
    Bruce Lipshutz; Fiscal Year: 2003
    ..abstract_text> ..
  14. Metal-Mediated Routes to Biaryls
    Bruce Lipshutz; Fiscal Year: 2004
    ..A particular, albeit representative, application of a novel substituted cyclo-NOBIN will be studied for selected asymmetric aldol reactions. ..
  15. Serotonin and CRF Pathways in Anxiety & HPA Regulation
    Anantha Shekhar; Fiscal Year: 2004
    ....
  16. NEUROLEPTIC SPACER LENGTH GOVERNS MOLECULAR RECOGNITION
    John Schetz; Fiscal Year: 2002
    ..Only positions 2.53, 2.60, 2.62, and 2.64 on serotonin receptors will be considered, because these are the only positions in TMS2 that are believed to be facing the binding pocket and that have different amino acids for the two subtypes...
  17. NATURALLY OCCURRING POLYENES VIA ORGANOMETALLICS
    Bruce Lipshutz; Fiscal Year: 2003
    ..abstract_text> ..
  18. A mechanism for TNF induced endothelial dysfunction
    Arnold Johnson; Fiscal Year: 2007
    ..abstract_text> ..
  19. Muscarinic agonists for neurological disorders
    William Messer; Fiscal Year: 2007
    ..The studies outlined here will provide new approaches for the treatment of neurological disorders, including Alzheimer's disease and schizophrenia. ..
  20. Selective in vivo Ablation of Leukemia Stem Cells
    Craig Jordan; Fiscal Year: 2007
    ..Collectively, the proposed studies will provide a detailed evaluation of how therapeutic agents impact the growth and survival of LSC in vivo. ..
  21. Role of Serotonin and CRF Pathways in Anxiety and HPA Regulations
    ANANTHA contact SHEKHAR; Fiscal Year: 2010
    ..The results of these studies could position us to develop novel genetically-targeted treatments and prevention strategies for chronic disabling illnesses such as panic and social anxiety disorder. ..
  22. NEUROLEPTIC SPACER LENGTH GOVERNS MOLECULAR RECOGNITION
    John Schetz; Fiscal Year: 2009
    ....
  23. Neurobiology of Anxiety and Panic Disorders
    Anantha Shekhar; Fiscal Year: 2010
    ..Finally, we will study the role of local versus extrinsic GABA neurons by GAD-67/65 gene silencing in the DMH/PeF region. ..
  24. Role of Serotonin and CRF Pathways in Anxiety and HPA Regulations
    Anantha Shekhar; Fiscal Year: 2009
    ..The results of these studies could position us to develop novel genetically-targeted treatments and prevention strategies for chronic disabling illnesses such as panic and social anxiety disorder. ..
  25. New Technologies for Catalysis in Water
    Bruce Lipshutz; Fiscal Year: 2009
    ..This technology also is to be applied to other important cross-couplings, such as aminations and asymmetric additions of hydride to Michael acceptors, all in water at room temperature. ..
  26. Selective in vivo Ablation of Leukemia Stem Cells
    Craig Jordan; Fiscal Year: 2009
    ..Collectively, the proposed studies will provide a detailed evaluation of how therapeutic agents impact the growth and survival of LSC in vivo. ..
  27. New Technologies for Catalysis in Water
    Bruce H Lipshutz; Fiscal Year: 2010
    ..This technology also is to be applied to other important cross-couplings, such as aminations and asymmetric additions of hydride to Michael acceptors, all in water at room temperature. ..
  28. Selective in vivo Ablation of Leukemia Stem Cells
    Craig Jordan; Fiscal Year: 2008
    ..Collectively, the proposed studies will provide a detailed evaluation of how therapeutic agents impact the growth and survival of LSC in vivo. ..
  29. A mechanism for TNF induced endothelial dysfunction
    Arnold Johnson; Fiscal Year: 2007
    ..abstract_text> ..
  30. Amnis ImageStream Flow Cytometer
    Craig Jordan; Fiscal Year: 2007
    ..Taken together, the unique capabilities of the ImageStream system will therefore serve to strongly benefit a wide range of research activities. [unreadable] [unreadable] [unreadable]..
  31. A mechanism for TNF induced endothelial dysfunction
    Arnold Johnson; Fiscal Year: 2008
    ..abstract_text> ..
  32. Neurobiology of Anxiety and Panic Disorders
    Anantha Shekhar; Fiscal Year: 2007
    ..Finally, we will study the role of local versus extrinsic GABA neurons by GAD-67/65 gene silencing in the DMH/PeF region. ..
  33. Cellular and Molecular Studies of Leukemic Stem Cellss
    Craig Jordan; Fiscal Year: 2003
    ..Collectively, these efforts will advance our understanding of basic mechanisms that underlie leukemic transformation and will improve strategies for the preferential ablation of LSCs. ..
  34. FINE TUNING BINOLS AND BINAPS FOR ASYMMETRIC SYNTHESIS
    Bruce Lipshutz; Fiscal Year: 2001
    ..From ligands of this type come further options, such as opportunities for polymer mounting, and potentially of greatest attention, conversion to substituted cyclo BINAPs. ..
  35. NATURALLY OCCURRING POLYENES VIA ORGANOMETALLICS
    Bruce Lipshutz; Fiscal Year: 2001
    ..abstract_text> ..
  36. FINE TUNING BINOLS AND BINAPS FOR ASYMMETRIC SYNTHESIS
    Bruce Lipshutz; Fiscal Year: 1999
    ..From ligands of this type come further options, such as opportunities for polymer mounting, and potentially of greatest attention, conversion to substituted cyclo BINAPs. ..
  37. NATURALLY OCCURRING POLYENES VIA ORGANOMETALLICS
    Bruce Lipshutz; Fiscal Year: 2000
    ..abstract_text> ..
  38. DEVELOPMENT OF NOVEL MUSCARINIC AGONISTS
    William Messer; Fiscal Year: 2000
    ..In addition the research could provide new approaches to the synthesis of compounds useful in a variety of neurological disorders. ..
  39. NATURALLY OCCURRING POLYENES VIA ORGANOMETALLICS
    Bruce Lipshutz; Fiscal Year: 1999
    ..abstract_text> ..
  40. DEVELOPMENT OF NOVEL MUSCARINIC AGONISTS
    William Messer; Fiscal Year: 1999
    ..In addition the research could provide new approaches to the synthesis of compounds useful in a variety of neurological disorders. ..
  41. FINE TUNING BINOLS AND BINAPS FOR ASYMMETRIC SYNTHESIS
    Bruce Lipshutz; Fiscal Year: 2000
    ..From ligands of this type come further options, such as opportunities for polymer mounting, and potentially of greatest attention, conversion to substituted cyclo BINAPs. ..
  42. NATURALLY OCCURRING POLYENES VIA ORGANOMETALLICS
    Bruce Lipshutz; Fiscal Year: 1999
    ....
  43. NATURALLY OCCURRING POLYENES VIA ORGANOMETALLICS
    Bruce Lipshutz; Fiscal Year: 2000
    ..abstract_text> ..
  44. NOVEL ORGANOMETALLIC ROUTES TO POLYENES & DERIVATIVES
    Bruce Lipshutz; Fiscal Year: 1993
    ..Further extension of this new chemistry to the direct preparation of homochiral C-4-substituted (dideoxy) riboses is also envisioned...
  45. NOVEL ORGANOMETALLIC ROUTES TO POLYENES & DERIVATIVES
    Bruce Lipshutz; Fiscal Year: 1992
    ..Further extension of this new chemistry to the direct preparation of homochiral C-4-substituted (dideoxy) riboses is also envisioned...
  46. Serotonin and CRF Pathways in Anxiety & HPA Regulation
    Anantha Shekhar; Fiscal Year: 2003
    ....
  47. NO & AP-1 MODULATE TNF-ACTIVATED LUNG ENDOTHELIAL PROTEI
    Arnold Johnson; Fiscal Year: 2002
    ..Synthesis of PKC-alpha is studied using immunoprecipitation and Western Blot of 35S-labeled PKC, and activity of PKC is assessed by PKC translocation and phosphorylation of PKC-alpha specific substrate. ..
  48. NATURALLY OCCURRING POLYENES VIA ORGANOMETALLICS
    Bruce Lipshutz; Fiscal Year: 2002
    ..abstract_text> ..
  49. Cellular and Molecular Studies of Leukemic Stem Cellss
    Craig Jordan; Fiscal Year: 2002
    ..Collectively, these efforts will advance our understanding of basic mechanisms that underlie leukemic transformation and will improve strategies for the preferential ablation of LSCs. ..
  50. NO & AP-1 MODULATE TNF-ACTIVATED LUNG ENDOTHELIAL PROTEI
    Arnold Johnson; Fiscal Year: 2001
    ..Synthesis of PKC-alpha is studied using immunoprecipitation and Western Blot of 35S-labeled PKC, and activity of PKC is assessed by PKC translocation and phosphorylation of PKC-alpha specific substrate. ..
  51. Neurobiology of Anxiety and Panic Disorders
    Anantha Shekhar; Fiscal Year: 2008
    ..Finally, we will study the role of local versus extrinsic GABA neurons by GAD-67/65 gene silencing in the DMH/PeF region. ..
  52. Neurobiology of Anxiety and Panic Disorders
    Anantha Shekhar; Fiscal Year: 2009
    ..Finally, we will study the role of local versus extrinsic GABA neurons by GAD-67/65 gene silencing in the DMH/PeF region. ..
  53. Neurobiology of Anxiety and Panic Disorders
    Anantha Shekhar; Fiscal Year: 2008
    ..Finally, we will study the role of local versus extrinsic GABA neurons by GAD-67/65 gene silencing in the DMH/PeF region. ..
  54. Cellular and Molecular Studies of Leukemic Stem Cellss
    Craig Jordan; Fiscal Year: 2004
    ..Collectively, these efforts will advance our understanding of basic mechanisms that underlie leukemic transformation and will improve strategies for the preferential ablation of LSCs. ..
  55. Serotonin and CRF Pathways in Anxiety & HPA Regulation
    Anantha Shekhar; Fiscal Year: 2005
    ....
  56. Cellular and Molecular Studies of Leukemic Stem Cellss
    Craig Jordan; Fiscal Year: 2005
    ..Collectively, these efforts will advance our understanding of basic mechanisms that underlie leukemic transformation and will improve strategies for the preferential ablation of LSCs. ..
  57. NEUROLEPTIC SPACER LENGTH GOVERNS MOLECULAR RECOGNITION
    John Schetz; Fiscal Year: 2003
    ....
  58. Serotonin and CRF Pathways in Anxiety & HPA Regulation
    Anantha Shekhar; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  59. NEUROLEPTIC SPACER LENGTH GOVERNS MOLECULAR RECOGNITION
    John Schetz; Fiscal Year: 2006
    ....
  60. NEUROLEPTIC SPACER LENGTH GOVERNS MOLECULAR RECOGNITION
    John Schetz; Fiscal Year: 2007
    ....
  61. NEUROLEPTIC SPACER LENGTH GOVERNS MOLECULAR RECOGNITION
    John Schetz; Fiscal Year: 2003
    ....
  62. CYTOPROTECTIVE ROLE OF HSP72 IN RENAL CELL INJURY
    STEVEN BORKAN; Fiscal Year: 2007
    ..These insights can prompt the development of preemptive strategies for preventing renal cell injury during ischemic insults as well as other forms of renal injury in which apoptosis contributes to organ failure. ..
  63. CYTOPROTECTIVE ROLE OF HSP72 IN RENAL CELL INJURY
    STEVEN BORKAN; Fiscal Year: 2004
    ..These insights can prompt the development of preemptive strategies for preventing renal cell injury during ischemic insults as well as other forms of renal injury in which apoptosis contributes to organ failure. ..
  64. CYTOPROTECTIVE ROLE OF HSP 72 IN RENAL CELL INJURY
    STEVEN BORKAN; Fiscal Year: 2002
    ..abstract_text> ..
  65. CYTOPROTECTIVE ROLE OF HSP72 IN RENAL CELL INJURY
    STEVEN BORKAN; Fiscal Year: 2003
    ..These insights can prompt the development of preemptive strategies for preventing renal cell injury during ischemic insults as well as other forms of renal injury in which apoptosis contributes to organ failure. ..
  66. CYTOPROTECTIVE ROLE OF HSP72 IN RENAL CELL INJURY
    STEVEN BORKAN; Fiscal Year: 2006
    ..These insights can prompt the development of preemptive strategies for preventing renal cell injury during ischemic insults as well as other forms of renal injury in which apoptosis contributes to organ failure. ..
  67. CYTOPROTECTIVE ROLE OF HSP 72 IN RENAL CELL INJURY
    STEVEN BORKAN; Fiscal Year: 1999
    ..abstract_text> ..
  68. CYTOPROTECTIVE ROLE OF HSP 72 IN RENAL CELL INJURY
    STEVEN BORKAN; Fiscal Year: 2001
    ..abstract_text> ..
  69. CYTOPROTECTIVE ROLE OF HSP 72 IN RENAL CELL INJURY
    STEVEN BORKAN; Fiscal Year: 2000
    ..abstract_text> ..
  70. CYTOPROTECTIVE ROLE OF HSP72 IN RENAL CELL INJURY
    STEVEN BORKAN; Fiscal Year: 2005
    ..These insights can prompt the development of preemptive strategies for preventing renal cell injury during ischemic insults as well as other forms of renal injury in which apoptosis contributes to organ failure. ..