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

Add time:07/14/2019    Source:sciencedirect.com

A series of 2-sulfonamidopyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamide were investigated as hTRPV1 ligands. Systematic modification on the 2-sulfonamido group provided highly potent TRPV1 antagonists. The N-benzyl phenylsulfonamide derivatives 12 and 23 in particular showed higher affinities than that of lead compound 1. Compound 12 exhibited strong analgesic activity in the formalin pain model. Docking analysis of its chiral S-form 12S in our hTRPV1 homology model indicated that its high affinity might arise from additional hydrophobic interactions not present in lead compound 1S.

We also recommend Trading Suppliers and Manufacturers of 4-METHOXY-2-[(4-METHYLBENZYL)AMINO]NICOTINONITRILE (cas 339102-90-8). Pls Click Website Link as below: cas 339102-90-8 suppliers

Prev:The Candida rugosa lipase catalyzed synthesis of AMYL ISOBUTYRATE (cas 2445-72-9) in organic solvent and solvent-free system: A kinetic study
Next:Hierarchical batch-to-batch optimization of cobalt oxalate synthesis process based on data-driven model)