935517-00-3Relevant academic research and scientific papers
2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4- methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists
Ryu, Hyungchul,Seo, Sejin,Kim, Myeong Seop,Kim, Mi-Yeon,Kim, Ho Shin,Ann, Jihyae,Tran, Phuong-Thao,Hoang, Van-Hai,Byun, Jieun,Cui, Minghua,Son, Karam,Sharma, Pankaz Kumar,Choi, Sun,Blumberg, Peter M.,Frank-Foltyn, Robert,Bahrenberg, Gregor,Koegel, Babette-Yvonne,Christoph, Thomas,Frormann, Sven,Lee, Jeewoo
, p. 4044 - 4047 (2014/09/03)
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.
