Synthesis and preliminary pharmacological evaluation of new analogues of diclofenac as potential anti-inflammatory agents

Abstract EN

A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential antiinflammatory agents with expected COX-2 selectivity.

In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg / Kg) of diclofenac sodium.

All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v / v (control group).

Moreover, the 4-aminobenzenesulfonamide derivative (compound 9) exhibited superior antiinflammatory activity compared to diclofenac sodium at times 180-300 minutes with the same onset of action.

The results of this study indicate that the incorporation of the selected aromatic amino groups in to diclofenac maintain its anti-inflammatory activity.