1.
Bioorg Med Chem Lett
; 18(20): 5609-13, 2008 Oct 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18809327
RESUMO
6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the discovery of 6-(4-fluorophenyl)-2-methyl-N-(2-methylbenzothiazol-5-yl)nicotinamide (32; SB-782443) which possesses an excellent overall profile and has been progressed into pre-clinical development.