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Novel 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazones: Orally effective anti-inflammatory drug candidates

2008; Elsevier BV; Volume: 17; Issue: 3 Linguagem: Inglês

10.1016/j.bmc.2008.12.045

1464-3391

Jorge L. M. Tributino, Carolina D. Duarte, Rodrigo S. Corrêa, A.C. Doriguetto, Javier Ellena, Nelilma Correia Romeiro, Newton G. Castro, Ana Luísa P. Miranda, Eliezer J. Barreiro, Carlos Alberto Manssour Fraga,

Bioactive Compounds and Antitumor Agents

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 micromol/kg, acting mainly as a non-selective COX inhibitor.