- Levels and immunolocalization of endogenous cytokinins in thidiazuron-induced shoot organogenesis in carnation
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...
- Anticancer, neuroprotective activities and computational studies of 2-amino-1,3,4-thiadiazole based compound
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...
- GSK3beta promotes apoptosis after renal ischemic injury
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...
- GSK-3beta inhibitors attenuate the organ injury/dysfunction caused by endotoxemia in the rat
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...
- Inhibition of gamma-secretase activity inhibits tumor progression in a mouse model of pancreatic ductal adenocarcinoma
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...
- Inhibiting glycogen synthase kinase-3 reduces endotoxaemic acute renal failure by down-regulating inflammation and renal cell apoptosis
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...
- 5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone
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)...
- 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
- 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...
- Glycogen synthase kinase-3beta inhibitors protect against the organ injury and dysfunction caused by hemorrhage and resuscitation
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...
- 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
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...
- Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles
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...
- Synthesis and in-vitro anticancer activity of 3,5-bis(indolyl)-1,2,4-thiadiazoles
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...
- Synthesis and antileishmanial activity of novel 5-(5-nitrofuran-2-y1)-1,3,4-thiadiazoles with piperazinyl-linked benzamidine substituents
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 ..
- 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
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...
- Synthesis and in vitro leishmanicidal activity of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles
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...
- 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...
- Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies
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...
- 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
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...
- 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...
- 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
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...
- Synthesis and anticancer activity of 5-(3-indolyl)-1,3,4-thiadiazoles
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...
- 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 ..
- Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles
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..
- 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...
- 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...
- Synthesis and antiviral activity evaluation of some new 6-substituted 3-(1-adamantyl)-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles
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...
- 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
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 ..
- 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...
- 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...
- Synthesis and anti-inflammatory activity of 1-acylthiosemicarbazides, 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazole-3-thiones
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)...
- Inhibition of glycogen synthase kinase-3beta attenuates the development of carrageenan-induced lung injury in mice
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...
- First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease
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...
- Glycogen synthase kinase-3 beta inhibition reduces secondary damage in experimental spinal cord trauma
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...
- Differences in kinetics of xanomeline binding and selectivity of activation of G proteins at M(1) and M(2) muscarinic acetylcholine receptors
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...
- 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...
- Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia
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...
- Growth control of multiple myeloma cells through inhibition of glycogen synthase kinase-3
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...
- Allosteric modulation by persistent binding of xanomeline of the interaction of competitive ligands with the M1 muscarinic acetylcholine receptor
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...
- 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...
- 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...
- 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
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...
- Glycogen synthase kinase-3beta inhibition attenuates the degree of arthritis caused by type II collagen in the mouse
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...
- Heterocyclic system containing bridgehead nitrogen atom: synthesis and pharmacological activities of some substituted 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles
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...
- 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...
- 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...
- 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...
- Role of receptor protein and membrane lipids in xanomeline wash-resistant binding to muscarinic M1 receptors
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...
- 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
- On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor
Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Minneapolis, Minnesota 55455, USA
Mol Pharmacol 53:1120-30. 1998
- Synthesis, antioxidant properties and radioprotective effects of new benzothiazoles and thiadiazoles
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...
- 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...
- 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...
- Insulin reduces cerebral ischemia/reperfusion injury in the hippocampus of diabetic rats: a role for glycogen synthase kinase-3beta
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...
- Benzothiadiazole, a novel class of inducers of systemic acquired resistance, activates gene expression and disease resistance in wheat
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...
- Effect of a new 1,3,4-thiadiazolium mesoionic compound (MI-D) on B16-F10 murine melanoma
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...
- 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...
- Novel persistent activation of muscarinic M1 receptors by xanomeline
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...
- Synthesis and antiproliferative activity of some 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles
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...
- NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders
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...
- Antimelanoma activity of 1,3,4-thiadiazolium mesoionics: a structure-activity relationship study
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...
- Treatment with the glycogen synthase kinase-3beta inhibitor, TDZD-8, affects transient cerebral ischemia/reperfusion injury in the rat hippocampus
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...
- Environmentally sensitive, SA-dependent defense responses in the cpr22 mutant of Arabidopsis
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...
- The influence of growth regulators on shoot proliferation and rooting of in vitro propagated caper
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...
- TDZ, auxin and genotype effects on leaf organogenesis in Fragaria
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...
- [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...
- In vitro plant regeneration from leaf-derived callus of Cimicifuga racemosa
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...
- Transgenic studies on the involvement of cytokinin and gibberellin in male development
Mystic Research, Monsanto Company, St Louis, Missouri 63198, USA
Plant Physiol 131:1270-82. 2003
- 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
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...
- Correlation of epiphyllous bud differentiation with foliar senescence in crassulacean succulent Kalanchoe pinnata as revealed by thidiazuron and ethrel application
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...
- Involvement of phospholipases C and D in early response to SAR and ISR inducers in Brassica napus plants
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...
- 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...
- 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...
- 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
- Optimizing regeneration condition in chickpea (Cicer arietinum L.)
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...
- 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...
- Transgene expression in strawberries driven by a heterologous phloem-specific promoter
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...
- In vitro regeneration of Salix nigra from adventitious shoots
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...
- 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...
- 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...
- 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...
- High-frequency shoot multiplication in Curcuma longa L using thidiazuron
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...
- In vitro regeneration of Hagenia abyssinica (Bruce) J.F. Gmel. (Rosaceae) from leaf explants
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...
- Artemisinin production by shoot regeneration of Artemisia annua L. using thidiazuron
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...
- Thidiazuron induces shoot organogenesis at low concentrations and somatic embryogenesis at high concentrations on leaf and petiole explants of African violet (Saintpaulia ionantha Wendl)
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...
- Direct somatic embryogenesis and synthetic seed production from Paulownia elongata
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...
- In vitro micropropagation of Boswellia ovalifoliolata
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...
- Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations
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...
- 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...
- 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...
- 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...
- Synthesis and anticancer activity of a novel class of flavonoids: 2,4-diarylchromane[4,3-d]-delta(1,9b)-1,2,3-thiadiazolines
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...
- Novel aminopeptidase N inhibitors derived from 1,3,4-thiadiazole scaffold
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...
- 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
- [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-..
- 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...
- 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...
- Synthesis and evaluation of antitubercular activity of imidazo[2,1-b][1,3,4]thiadiazole derivatives
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 ..
- 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...
- Synthesis and antifungal activity of novel sulfoxide derivatives containing trimethoxyphenyl substituted 1,3,4-thiadiazole and 1,3,4-oxadiazole moiety
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...
- Synthesis and antibacterial activity of N-[5-(chlorobenzylthio)-1,3,4-thiadiazol-2-yl] piperazinyl quinolone derivatives
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...