Artículos de revistas
Novel 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazones: Orally effective anti-inflammatory drug candidates
Fecha
2009Registro en:
BIOORGANIC & MEDICINAL CHEMISTRY, v.17, n.3, p.1125-1131, 2009
0968-0896
10.1016/j.bmc.2008.12.045
Autor
TRIBUTINO, Jorge L. M.
DUARTE, Carolina D.
CORREA, Rodrigo S.
DORIGUETTO, Antonio C.
ELLENA, Javier
ROMEIRO, Nelilma C.
CASTRO, Newton G.
MIRANDA, Ana Luisa P.
BARREIRO, Eliezer J.
FRAGA, Carlos A. M.
Institución
Resumen
We described herein the molecular design of novel in vivo anti-inflammatory 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazone derivatives (1) planned by applying the molecular hybridization approach. This work also points out to the discovery of LASSBio-930 (1c) as a novel anti-inflammatory and anti-hyperalgesic prototype, which was able to reduce carrageenan-induced rat paw edema with an ED(50) of 97.8 mu mol/kg, acting mainly as a non-selective COX inhibitor. (C) 2009 Elsevier Ltd. All rights reserved.