PubMed 25659771

Referenced in Channelpedia wiki pages of: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.

Authors: HyungChul Ryu, Sejin Seo, Jee-Young Lee, Tae-Hwan Ha, Sunho Lee, Aeran Jung, Jihyae Ann, Sung-Eun Kim, Suyoung Yoon, Mannkyu Hong, Peter M Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Klaus Schiene, Hannelore Stockhausen, Thomas Christoph, Sven Frormann, Jeewoo Lee

Journal, date & volume: Eur J Med Chem, 2015 Mar 26 , 93, 101-8

PubMed link:

A series of pyridine derivatives in the C-region of N-((6-trifluoromethyl-pyridin-3-yl)methyl) 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. The SAR analysis indicated that 6-difluorochloromethyl pyridine derivatives were the best surrogates of the C-region for previous leads. Among them, compound 31 showed excellent antagonism to capsaicin as well as to multiple hTRPV1 activators. It demonstrated strong analgesic activity in the formalin test in mice with full efficacy and it blocked capsaicin-induced hypothermia in vivo.