@article{f34579db5a1747c8a8afe47308a7a117,
title = "2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4- methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists",
abstract = "A series of 2-aryl pyridine C-region derivatives of 2-(3-fluoro-4- methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Multiple compounds showed highly potent TRPV1 antagonism toward capsaicin comparable to previous lead 7. Among them, compound 9 demonstrated anti-allodynia in a mouse neuropathic pain model and blocked capsaicin-induced hypothermia in a dose-dependent manner. Docking analysis of 9 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 Kim, {Myeong Seop} and Kim, {Mi Yeon} and Kim, {Ho Shin} and Jihyae Ann and Tran, {Phuong Thao} and Hoang, {Van Hai} and Jieun Byun and Minghua Cui and Karam Son and Sharma, {Pankaz Kumar} and Sun Choi and Blumberg, {Peter M.} and Robert Frank-Foltyn and Gregor Bahrenberg and Koegel, {Babette Yvonne} and Thomas Christoph and Sven Frormann and Jeewoo Lee",
note = "Funding Information: We greatly acknowledge Elke Schumacher and Franz-Josef Butz for technical assistance in CCI and Cap hypothermia studies, resp. 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 (Project Z1A BC 005270), USA. ",
year = "2014",
month = aug,
day = "15",
doi = "10.1016/j.bmcl.2014.05.072",
language = "English",
volume = "24",
pages = "4044--4047",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Ltd.",
number = "16",
}