DSpace at EWHA: 6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists

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DC Field	Value	Language
dc.contributor.author	최선	*
dc.date.accessioned	2016-08-29T12:08:47Z	-
dc.date.available	2016-08-29T12:08:47Z	-
dc.date.issued	2015	*
dc.identifier.issn	0960-894X	*
dc.identifier.other	OAK-14521	*
dc.identifier.uri	https://dspace.ewha.ac.kr/handle/2015.oak/230404	-
dc.description.abstract	A series of N-[{2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)-pyridin-3-yl}methyl] N′-(6,6-fused heterocyclic) ureas have been investigated as hTRPV1 antagonists. Among them, compound 15 showed highly potent TRPV1 antagonism to capsaicin, with Ki(ant) = 0.2 nM, as well as antagonism to other activators, and it was efficacious in a pain model. A docking study of 15 with our hTRPV1 homology model indicates that there is crucial hydrogen bonding between the ring nitrogen and the receptor, contributing to its potency. © 2015 Elsevier Ltd. All rights reserved.	*
dc.language	English	*
dc.publisher	Elsevier Ltd	*
dc.subject	Analgesic	*
dc.subject	Molecular modeling	*
dc.subject	TRPV1 antagonist	*
dc.subject	Vanilloid receptor 1	*
dc.title	6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists	*
dc.type	Article	*
dc.relation.issue	4	*
dc.relation.volume	25	*
dc.relation.index	SCI	*
dc.relation.index	SCIE	*
dc.relation.index	SCOPUS	*
dc.relation.startpage	803	*
dc.relation.lastpage	806	*
dc.relation.journaltitle	Bioorganic and Medicinal Chemistry Letters	*
dc.identifier.doi	10.1016/j.bmcl.2014.12.086	*
dc.identifier.wosid	WOS:000349720400013	*
dc.identifier.scopusid	2-s2.0-84964203457	*
dc.author.google	Sun W.	*
dc.author.google	Kim H.-S.	*
dc.author.google	Lee S.	*
dc.author.google	Jung A.	*
dc.author.google	Kim S.-E.	*
dc.author.google	Ann J.	*
dc.author.google	Yoon S.	*
dc.author.google	Choi S.	*
dc.author.google	Lee J.H.	*
dc.author.google	Blumberg P.M.	*
dc.author.google	Frank-Foltyn R.	*
dc.author.google	Bahrenberg G.	*
dc.author.google	Schiene K.	*
dc.author.google	Stockhausen H.	*
dc.author.google	Christoph T.	*
dc.author.google	Frormann S.	*
dc.author.google	Lee J.	*
dc.contributor.scopusid	최선(8659831000)	*
dc.date.modifydate	20240305081003	*