@article{43fc1b5188184dffa0f6ffd430cdb58c,
title = "6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists",
abstract = "A series of N-[{2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)-pyridin-3-yl}methyl] N′-(6,6-fused heterocyclic) ureas have been investigated as hTRPV1 antagonists. Among them, compound 15 showed highly potent TRPV1 antagonism to capsaicin, with Ki(ant) = 0.2 nM, as well as antagonism to other activators, and it was efficacious in a pain model. A docking study of 15 with our hTRPV1 homology model indicates that there is crucial hydrogen bonding between the ring nitrogen and the receptor, contributing to its potency.",
keywords = "Analgesic, Molecular modeling, TRPV1 antagonist, Vanilloid receptor 1",
author = "Wei Sun and Kim, {Hyo Shin} and Sunho Lee and Aeran Jung and Kim, {Sung Eun} and Jihyae Ann and Suyoung Yoon and Sun Choi and Lee, {Jin Hee} and Blumberg, {Peter M.} and Robert Frank-Foltyn and Gregor Bahrenberg and Klaus Schiene and Hannelore Stockhausen and Thomas Christoph and Sven Frormann and Jeewoo Lee",
note = "Funding Information: This research was supported by Grants from Grunenthal , the Korea Health Technology R&D Project (HI13D2358), National Research Foundation of Korea ( R11-2007-107-02001-0 ), the National Leading Research Lab Program (2011-0028885), and in part by the Intramural Research Program of NIH, Center for Cancer Research, NCI (Project Z1A BC 005270). Publisher Copyright: {\textcopyright} 2015 Elsevier Ltd. All rights reserved.",
year = "2015",
month = feb,
day = "15",
doi = "10.1016/j.bmcl.2014.12.086",
language = "English",
volume = "25",
pages = "803--806",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Ltd.",
number = "4",
}