DSpace at EWHA: 2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists

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DC Field	Value	Language
dc.contributor.author	최선	*
dc.date.accessioned	2016-08-29T12:08:05Z	-
dc.date.available	2016-08-29T12:08:05Z	-
dc.date.issued	2016	*
dc.identifier.issn	0968-0896	*
dc.identifier.other	OAK-16515	*
dc.identifier.uri	https://dspace.ewha.ac.kr/handle/2015.oak/231103	-
dc.description.abstract	A series of 2-sulfonamidopyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamide were investigated as hTRPV1 ligands. Systematic modification on the 2-sulfonamido group provided highly potent TRPV1 antagonists. The N-benzyl phenylsulfonamide derivatives 12 and 23 in particular showed higher affinities than that of lead compound 1. Compound 12 exhibited strong analgesic activity in the formalin pain model. Docking analysis of its chiral S-form 12S in our hTRPV1 homology model indicated that its high affinity might arise from additional hydrophobic interactions not present in lead compound 1S. © 2016 Elsevier Ltd. All rights reserved.	*
dc.language	English	*
dc.publisher	Elsevier Ltd	*
dc.subject	Analgesic	*
dc.subject	TRPV1 antagonists	*
dc.subject	Vanilloid receptor 1	*
dc.title	2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists	*
dc.type	Article	*
dc.relation.issue	6	*
dc.relation.volume	24	*
dc.relation.index	SCI	*
dc.relation.index	SCIE	*
dc.relation.index	SCOPUS	*
dc.relation.startpage	1231	*
dc.relation.lastpage	1240	*
dc.relation.journaltitle	Bioorganic and Medicinal Chemistry	*
dc.identifier.doi	10.1016/j.bmc.2016.01.051	*
dc.identifier.wosid	WOS:000370822700009	*
dc.identifier.scopusid	2-s2.0-84958897541	*
dc.author.google	Ann J.	*
dc.author.google	Ki Y.	*
dc.author.google	Yoon S.	*
dc.author.google	Kim M.S.	*
dc.author.google	Lee J.-U.	*
dc.author.google	Kim C.	*
dc.author.google	Lee S.	*
dc.author.google	Jung A.	*
dc.author.google	Baek J.	*
dc.author.google	Hong S.	*
dc.author.google	Choi S.	*
dc.author.google	Pearce L.V.	*
dc.author.google	Esch T.E.	*
dc.author.google	Turcios N.A.	*
dc.author.google	Lewin N.E.	*
dc.author.google	Ogunjirin A.E.	*
dc.author.google	Herold B.K.A.	*
dc.author.google	McCall A.K.	*
dc.author.google	Blumberg P.M.	*
dc.author.google	Lee J.	*
dc.contributor.scopusid	최선(8659831000)	*
dc.date.modifydate	20240305081003	*