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dc.contributor.author부 호앙 남-
dc.contributor.author김지영-
dc.contributor.authorAhmed Helmy Ebraheem Hassan-
dc.contributor.author최기항-
dc.contributor.author박종현-
dc.contributor.author박기덕-
dc.contributor.author이재균-
dc.contributor.author배애님-
dc.contributor.author추현아-
dc.contributor.author민선준-
dc.contributor.author조용서-
dc.date.accessioned2015-12-03T02:08:56Z-
dc.date.available2015-12-03T02:08:56Z-
dc.date.issued201511-
dc.identifier.citationVOL 게재예정, 게재예정-
dc.identifier.issn0960894X-
dc.identifier.other45340-
dc.identifier.urihttp://pubs.kist.re.kr/handle/201004/50951-
dc.description.abstractWe described here the synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as potential mGluR5 antagonists. We found that a series of thiazole derivatives 6 showed better inhibitory activity against mGluR5. Compounds 6bc and 6bj have been identified as potent antagonists (IC50 = 274 and 159 nM) showing excellent in vitro stability profile. Molecular docking study using the crystal structure of mGluR5 revealed that our compounds 6bc and 6bj fit the allosteric binding site of mavoglurant well.-
dc.publisherBioorganic & medicinal chemistry letters-
dc.subjectmetabotropic glutamate receptor-
dc.subjectantagonist-
dc.subjectpicolinamides-
dc.subjectthiazole-2- carboxamides-
dc.subjectmolecular docking-
dc.titleSynthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists-
dc.typeArticle-
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