Synthesis and Evaluation of Anti-inflammatory Activity of Some Chalcone Hydrazide Derivatives

Abstract

Aim: Chalcones are part of the selected group of chemical compounds related with diverse pharmacological activities such as antimicrobial, antiviral, antitumor, convulsion, anxiety, anti-inflammatory, andanalgesic. The aim of this study was to synthesize chalcones hydrazide derivatives and to evaluate their anti-inflammatory activity in the model of carrageenan induced edema in rats. Methods: The chalcone hydrazide derivatives were prepared by treating Isonicotinyl and Nicotinyl hydrazide with respective parent chalconeand environmentally friendly solvents with 78–85% yields in approximately 6 hrs. These compounds were characterized by 1H NMR, 13C NMR and IR spectroscopy. The structures of synthesised derivatives were evaluated on biological activity at dose of 40 mg/kg and they showed anti-inflammatory protective effect by oral administration, this effect was time dependent. Results: All the derivatives were given satisfactory reaction yields that representing the efficiency of the employed synthetic route. In carrageenan-induced paw edema model, CL-2derivative showed most significant percentage of inhibition (61.97%) as compared to reference standard Indomethacin. Conclusion: Compound CL-2 was showed significant anti-inflammatory activity due to presence of electron donating groups like –CH3 on ring A and electron withdrawing group like NO2 on ring B at 4th position in isonicotinyl hydrazide derivative. All synthetic chalcone hydrazide derivatives may be considered as safer drugs for treating inflammatory conditions.