Synthesis, pharmacological evaluation and electrochemical studies of novel 6-nitro-3, 4-methylenedioxyphenyl-N-acylhydrazone derivatives: Discovery of LASSBio- …

…, DI Lacerda, MV Martins, MS Alexandre-Moreira…

Index: Duarte, Carolina D.; Tributino, Jorge L.M.; Lacerda, Daniel I.; Martins, Marina V.; Alexandre-Moreira, Magna S.; Dutra, Fernando; Bechara, Etelvino J.H.; De-Paula, Francine S.; Goulart, Marilia O.F.; Ferreira, Juliano; Calixto, Joao B.; Nunes, Marise P.; Bertho, Alvaro L.; Miranda, Ana Luisa P.; Barreiro, Eliezer J.; Fraga, Carlos A.M. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 6 p. 2421 - 2433

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Citation Number: 61

Abstract

We describe herein the discovery of LASSBio-881 (3c) as a novel in vivo antinociceptive, anti-inflammatory, and in vitro antiproliferative and antioxidant compound, with a cannabinoid ligand profile. We observed that LASSBio-881 (3c) was able to bind to CB1 receptors (71% at 100μM) and also to inhibit T-cell proliferation (66% at 10μM) probably by binding to CB2 receptors, in a non-proapoptotic manner, different from anandamide (1). It ...