DSpace at EWHA: 2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists

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DC Field	Value	Language
dc.contributor.author	최선	*
dc.date.accessioned	2021-08-12T16:32:29Z	-
dc.date.available	2021-08-12T16:32:29Z	-
dc.date.issued	2021	*
dc.identifier.issn	0960-894X	*
dc.identifier.other	OAK-29856	*
dc.identifier.uri	https://dspace.ewha.ac.kr/handle/2015.oak/258810	-
dc.description.abstract	A series consisting of 117 2-(halogenated phenyl) acetamide and propanamide analogs were investigated as TRPV1 antagonists. The structure–activity analysis targeting their three pharmacophoric regions indicated that halogenated phenyl A-region analogs exhibited a broad functional profile ranging from agonism to antagonism. Among the compounds, antagonists 28 and 92 exhibited potent antagonism toward capsaicin for hTRPV1 with Ki[CAP] = 2.6 and 6.9 nM, respectively. Further, antagonist 92 displayed promising analgesic activity in vivo in both phases of the formalin mouse pain model. A molecular modeling study of 92 indicated that the two fluoro groups in the A-region made hydrophobic interactions with the receptor. © 2021 Elsevier Ltd	*
dc.language	English	*
dc.publisher	Elsevier Ltd	*
dc.subject	Analgesic	*
dc.subject	TRPV1 Antagonist	*
dc.subject	Vanilloid Receptor 1	*
dc.title	2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists	*
dc.type	Article	*
dc.relation.volume	48	*
dc.relation.index	SCIE	*
dc.relation.index	SCOPUS	*
dc.relation.journaltitle	Bioorganic and Medicinal Chemistry Letters	*
dc.identifier.doi	10.1016/j.bmcl.2021.128266	*
dc.identifier.wosid	WOS:000684377000019	*
dc.identifier.scopusid	2-s2.0-85111013432	*
dc.author.google	Kang J.M.	*
dc.author.google	Kwon S.O.	*
dc.author.google	Ann J.	*
dc.author.google	Lee S.	*
dc.author.google	Kim C.	*
dc.author.google	Do N.	*
dc.author.google	Jeong J.J.	*
dc.author.google	Blumberg P.M.	*
dc.author.google	Ha H.	*
dc.author.google	Vu T.N.L.	*
dc.author.google	Yoon S.	*
dc.author.google	Choi S.	*
dc.author.google	Frank-Foltyn R.	*
dc.author.google	Lesch B.	*
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	20240305081003	*