lassbio-294 and Edema
lassbio-294 has been researched along with Edema* in 2 studies
Other Studies
2 other study(ies) available for lassbio-294 and Edema
| Article | Year |
|---|---|
Novel 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazones: orally effective anti-inflammatory drug candidates.
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. Topics: Administration, Oral; Animals; Anti-Inflammatory Agents, Non-Steroidal; Benzodioxoles; Carrageenan; Computer Simulation; Crystallography, X-Ray; Cyclooxygenase Inhibitors; Disease Models, Animal; Edema; Female; Hydrazones; Male; Rats; Rats, Wistar; Thermodynamics | 2009 |
Synthesis, pharmacological evaluation and electrochemical studies of novel 6-nitro-3,4-methylenedioxyphenyl-N-acylhydrazone derivatives: Discovery of LASSBio-881, a new ligand of cannabinoid receptors.
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 100microM) and also to inhibit T-cell proliferation (66% at 10microM) probably by binding to CB2 receptors, in a non-proapoptotic manner, different from anandamide (1). It was also demonstrated that LASSBio-881 (3c) had an important antioxidant profile toward free radicals (DPPH and hydroxyl), probably due to its particular redox behavior, which reflects the presence of both nitro and 3,5-di-tert-butyl-4-hydroxyphenyl sub-units, as demonstrated by cyclic voltammetry studies. In addition, we showed that these structural sub-units are essential for the observed pharmacological activity. Topics: Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Arachidonic Acid; Arachidonic Acids; Biphenyl Compounds; Brain; Cannabinoid Receptor Modulators; Carrageenan; Cell Proliferation; Edema; Endocannabinoids; Female; Formaldehyde; Free Radical Scavengers; Hydrazines; Hydrazones; Ligands; Male; Mice; Models, Molecular; Pain; Picrates; Polyunsaturated Alkamides; Pyridines; Rats; Rats, Wistar; Receptor, Cannabinoid, CB1; Receptor, Cannabinoid, CB2; Structure-Activity Relationship; Superoxides; T-Lymphocytes | 2007 |