Synthesis and In vitro Biological Activity Evaluation of Substituted Chalcones

Chalcones; Claisen-Schmidt Condensation; In vitro Biological Activity.

Abstract

Chalcones and its derivatives are gaining a great deal of attention due to their biological and molecular activities in humans with an ever increasing investigation by in vitro or preclinical studies. In this study, four substituted chalcone derivatives (I-IV) were successfully synthesized using the conventional Claisen-Schmidt condensation between various substituted aromatic ketones and aromatic aldehydes in the presence of aqueous sodium hydroxide. The synthesized compounds gave good yields between 72.5 – 81.8%. In vitro Anti-inflammatory, antimicrobial and antioxidant activities were conducted to evaluate compounds’ pharmacological efficacy. In the anti-inflammatory test, compound 1 was most active which exhibits 20.9 % Membrane Stabilization Effect at 50 mg/mL which is lower than Diclofenac used as the standard. At the concentration of 3.91 µg/mL, compounds III and IV were found to neutralize 50 % of the DPPH free radicals, while the lowest activity was found in compound II at the concentration of 68.7 µg/mL. All the synthesized compounds were found to possess moderate activity against the test organisms when compared to the standards. Chalcones should be explored more as scaffold pharmacophore agents.