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dc.contributor.author민선준-
dc.date.accessioned2018-03-19T05:30:31Z-
dc.date.available2018-03-19T05:30:31Z-
dc.date.issued2016-01-
dc.identifier.citationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v. 26, No. 1, Page. 140-144en_US
dc.identifier.issn0960-894X-
dc.identifier.issn1464-3405-
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0960894X15302213-
dc.identifier.urihttp://hdl.handle.net/20.500.11754/48924-
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. (C) 2015 Elsevier Ltd. All rights reserved.en_US
dc.description.sponsorshipThis research was supported by the Korea Institute of Science and Technology (KIST, 2E25580, 2E25473, 2E25240, 2V03970) and by a Grant of the National Research Foundation of Korea (NRF-2013R1A1A2005550 and NRF-2015M3A9A8030034) funded by the Ministry of Science, ICT and Future Planning.en_US
dc.language.isoen_USen_US
dc.publisherPERGAMON-ELSEVIER SCIENCE LTDen_US
dc.subjectMetabotropic glutamate receptoren_US
dc.subjectAntagonisten_US
dc.subjectPicolinamidesen_US
dc.subjectThiazole-2-carboxamidesen_US
dc.subjectMolecular dockingen_US
dc.subjectNEGATIVE ALLOSTERIC MODULATORSen_US
dc.subjectGASTROESOPHAGEAL-REFLUX DISEASEen_US
dc.subjectFRAGILE-X-SYNDROMEen_US
dc.subjectNEUROPATHIC PAINen_US
dc.subjectPHARMACOLOGYen_US
dc.subjectMGLU(5)en_US
dc.subjectRATSen_US
dc.subjectIDENTIFICATIONen_US
dc.subjectSYMPTOMSen_US
dc.subjectEXPOSUREen_US
dc.titleSynthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonistsen_US
dc.typeArticleen_US
dc.relation.no1-
dc.relation.volume26-
dc.identifier.doi10.1016/j.bmcl.2015.11.012-
dc.relation.page140-144-
dc.relation.journalBIOORGANIC & MEDICINAL CHEMISTRY LETTERS-
dc.contributor.googleauthorVu, Hoang Nam-
dc.contributor.googleauthorKim, Ji Young-
dc.contributor.googleauthorHassan, Ahmed H. E-
dc.contributor.googleauthorChoi, Kihang-
dc.contributor.googleauthorPark, Jong-Hyun-
dc.contributor.googleauthorPark, Ki Duk-
dc.contributor.googleauthorLee, Jae Kyun-
dc.contributor.googleauthorPae, Ae Nim-
dc.contributor.googleauthorChoo, Hyunah-
dc.contributor.googleauthorMin, Sun-Joon-
dc.contributor.googleauthorCho, Yong Seo-
dc.relation.code2016000607-
dc.sector.campusE-
dc.sector.daehakCOLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E]-
dc.sector.departmentDEPARTMENT OF CHEMICAL AND MOLECULAR ENGINEERING-
dc.identifier.pidsjmin-
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