@article{085fd899b7b949718ad94af669a44ae5,
title = "α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists",
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 Ki(CAP) = 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.",
keywords = "Analgesic, Capsaicin, Molecular modeling, TRPV1 antagonist",
author = "Tran, {Phuong Thao} and Kim, {Ho Shin} and Jihyae Ann and Kim, {Sung Eun} and Changhoon Kim and Mannkyu Hong and Hoang, {Van Hai} and Ngo, {Van T.H.} and Sunhye Hong and Minghua Cui and Sun Choi and Blumberg, {Peter M.} and Robert Frank-Foltyn and Gregor Bahrenberg and Hannelore Stockhausen and Thomas Christoph and Jeewoo Lee",
note = "Funding Information: This research was supported by Research Grants from Grunenthal in Germany, Grants from the Korea Science and Engineering Foundation (KOSEF) ( NRF-2014M3A9B5073755 ) and National Leading Research Lab ( NLRL ) program ( 2011-0028885 ) in South Korea, and in part by the Intramural Research Program of NIH , Center for Cancer Research, NCI (Project Z1A BC 005270) in USA. Publisher Copyright: {\textcopyright} 2015 Elsevier Ltd. All rights reserved.",
year = "2015",
month = jun,
day = "1",
doi = "10.1016/j.bmcl.2015.04.024",
language = "English",
volume = "25",
pages = "2326--2330",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Ltd.",
number = "11",
}