@article{fe5dbde0ddfe4f61b70f9f5aaff35e4b,
title = "2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists",
abstract = "A series of 2-alkyl/alkenyl pyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Multiple compounds showed excellent and stereospecific TRPV1 antagonism with better potency than previous lead 2. Among them, compound 15f demonstrated a strong analgesic profile in a rat neuropathic pain model and blocked capsaicin-induced hypothermia in a dose-dependent manner. Docking analysis of (S)-15f with our hTRPV1 homology model provided insight into its specific binding mode.",
keywords = "Capsaicin, Molecular modeling, Resiniferatoxin, TRPV1 antagonist, Vanilloid receptor 1",
author = "Hyungchul Ryu and Sejin Seo and Cho, {Seong Hee} and Kim, {Ho Shin} and Aeran Jung and Kang, {Dong Wook} and Karam Son and Minghua Cui and Hong, {Sun Hye} and Sharma, {Pankaz Kumar} and Sun Choi and Blumberg, {Peter M.} and Robert Frank-Foltyn and Gregor Bahrenberg and Hannelore Stockhausen and Klaus Schiene and Thomas Christoph and Sven Frormann and Jeewoo Lee",
note = "Funding Information: This research was supported by Research Grants from Grunenthal, Germany, Grants from the National Research Foundation of Korea (NRF) ( R11-2007-107-02001-0 ), Grants from the National Leading Research Lab (NLRL) program ( 2011-0028885 ), Republic of Korea and in part by the Intramural Research Program of NIH , Center for Cancer Research, NCI, USA (Project Z1A BC 005270).",
year = "2014",
month = aug,
day = "15",
doi = "10.1016/j.bmcl.2014.05.074",
language = "English",
volume = "24",
pages = "4039--4043",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Ltd.",
number = "16",
}