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

Add time:07/21/2019    Source:sciencedirect.com

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.

We also recommend Trading Suppliers and Manufacturers of 2-(1-Methyl-piperidin-3-ylMethoxy)-ethanol (cas 112391-02-3). Pls Click Website Link as below: cas 112391-02-3 suppliers

Prev:Synthesis and biological evaluation of substituted 2-anilino-7H-pyrrolopyrimidines as PDK1 inhibitors
Next:Effects of zolpidem/Triazolam (cas 112393-65-4) on cognitive performance 12 hours after acute administration)