DSpace at EWHA: α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists

Browse

My Repository

View : 1104 Download: 0

Full metadata record

DC Field	Value	Language
dc.contributor.author	최선	*
dc.date.accessioned	2016-08-29T12:08:02Z	-
dc.date.available	2016-08-29T12:08:02Z	-
dc.date.issued	2015	*
dc.identifier.issn	0960-894X	*
dc.identifier.other	OAK-14868	*
dc.identifier.uri	https://dspace.ewha.ac.kr/handle/2015.oak/230542	-
dc.description.abstract	A series of α-substituted acetamide derivatives of previously reported 2-(3-fluoro-4-methylsulfonamidophenyl)propanamide leads (1, 2) were investigated for antagonism of hTRPV1 activation by capsaicin. Compound 34, which possesses an α-m-tolyl substituent, showed highly potent and selective antagonism of capsaicin with K<inf>i(CAP)</inf> = 0.1 nM. It thus reflected a 3-fold improvement in potency over parent 1. Docking analysis using our homology model indicated that the high potency of 34 might be attributed to a specific hydrophobic interaction of the m-tolyl group with the receptor. © 2015 Elsevier Ltd. All rights reserved.	*
dc.language	English	*
dc.publisher	Elsevier Ltd	*
dc.subject	Analgesic	*
dc.subject	Capsaicin	*
dc.subject	Molecular modeling	*
dc.subject	TRPV1 antagonist	*
dc.title	α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists	*
dc.type	Article	*
dc.relation.issue	11	*
dc.relation.volume	25	*
dc.relation.index	SCI	*
dc.relation.index	SCIE	*
dc.relation.index	SCOPUS	*
dc.relation.startpage	2326	*
dc.relation.lastpage	2330	*
dc.relation.journaltitle	Bioorganic and Medicinal Chemistry Letters	*
dc.identifier.doi	10.1016/j.bmcl.2015.04.024	*
dc.identifier.wosid	WOS:000354115400012	*
dc.identifier.scopusid	2-s2.0-84937762903	*
dc.author.google	Tran P.-T.	*
dc.author.google	Kim H.S.	*
dc.author.google	Ann J.	*
dc.author.google	Kim S.-E.	*
dc.author.google	Kim C.	*
dc.author.google	Hong M.	*
dc.author.google	Hoang V.-H.	*
dc.author.google	Ngo V.T.H.	*
dc.author.google	Hong S.	*
dc.author.google	Cui M.	*
dc.author.google	Choi S.	*
dc.author.google	Blumberg P.M.	*
dc.author.google	Frank-Foltyn R.	*
dc.author.google	Bahrenberg G.	*
dc.author.google	Stockhausen H.	*
dc.author.google	Christoph T.	*
dc.author.google	Lee J.	*
dc.contributor.scopusid	최선(8659831000)	*
dc.date.modifydate	20260622153104	*