1.
Bioorg Med Chem Lett
; 20(22): 6812-5, 2010 Nov 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-20855211
RESUMEN
A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Na(v)1.8 sodium channel is reported. Replacement of the furan nucleus and homologation of the anilide linker in subtype-selective blocker A-803467 (1) provided potent, selective derivatives with improved aqueous solubility and oral bioavailability. Representative compounds from this series displayed efficacy in rat models of inflammatory and neuropathic pain.