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약학대학
약학과
Journal papers
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α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists
Title
α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists
Authors
Tran P.-T.
;
Kim H.S.
;
Ann J.
;
Kim S.-E.
;
Kim C.
;
Hong M.
;
Hoang V.-H.
;
Ngo V.T.H.
;
Hong S.
;
Cui M.
;
Choi S.
;
Blumberg P.M.
;
Frank-Foltyn R.
;
Bahrenberg G.
;
Stockhausen H.
;
Christoph T.
;
Lee J.
Ewha Authors
최선
SCOPUS Author ID
최선
Issue Date
2015
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894X
Citation
Bioorganic and Medicinal Chemistry Letters vol. 25, no. 11, pp. 2326 - 2330
Keywords
Analgesic
;
Capsaicin
;
Molecular modeling
;
TRPV1 antagonist
Publisher
Elsevier Ltd
Indexed
SCI; SCIE; SCOPUS
Document Type
Article
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.
DOI
10.1016/j.bmcl.2015.04.024
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