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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
최선scopus
Issue Date
2015
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 25, no. 11, pp. 2326 - 2330
Keywords
AnalgesicCapsaicinMolecular modelingTRPV1 antagonist
Publisher
Elsevier Ltd
Indexed
SCI; SCIE; SCOPUS WOS scopus
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
Appears in Collections:
약학대학 > 약학과 > Journal papers
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