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

Add time:08/22/2019    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 3-FLUORO-4-(TRIFLUOROMETHYL)PYRIDINE (cas 113770-87-9). Pls Click Website Link as below: cas 113770-87-9 suppliers

Prev:Scavenging effect of nicorandil on free radicals and lipid peroxide in streptozotocin-induced diabetic rats*
Next:Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists)