1622453-18-2Relevant academic research and scientific papers
2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists
Ryu, Hyungchul,Seo, Sejin,Cho, Seong-Hee,Kim, Ho Shin,Jung, Aeran,Kang, Dong Wook,Son, Karam,Cui, Minghua,Hong, Sun-Hye,Sharma, Pankaz Kumar,Choi, Sun,Blumberg, Peter M.,Frank-Foltyn, Robert,Bahrenberg, Gregor,Stockhausen, Hannelore,Schiene, Klaus,Christoph, Thomas,Frormann, Sven,Lee, Jeewoo
, p. 4039 - 4043 (2014/09/16)
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.
