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

Title
2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists
Authors
Ann J.Ki Y.Yoon S.Kim M.S.Lee J.-U.Kim C.Lee S.Jung A.Baek J.Hong S.Choi S.Pearce L.V.Esch T.E.Turcios N.A.Lewin N.E.Ogunjirin A.E.Herold B.K.A.McCall A.K.Blumberg P.M.Lee J.
Ewha Authors
최선
SCOPUS Author ID
최선scopus
Issue Date
2016
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 24, no. 6, pp. 1231 - 1240
Keywords
AnalgesicTRPV1 antagonistsVanilloid receptor 1
Publisher
Elsevier Ltd
Indexed
SCI; SCIE; SCOPUS WOS scopus
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.
DOI
10.1016/j.bmc.2016.01.051
Appears in Collections:
약학대학 > 약학과 > Journal papers
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