Synthesis and preliminary pharmacological evaluation of aminobenzensulfonamides derivatives of mefenamic acid as a potential anti-inflammatory agents

Abstract EN

A group of amino derivatives [4-aminobenzenesulfonamide, 4-amino-N¹ methylbenzenesulfonamide, or N¹-(4-aminophenylsulfonyl) acetamide] bound to carboxyl group of mefenamic acid a well known nonsteroidal anti-inflammatory drugs (NSAIDs) were designed and synthesized for evaluation as a potential anti-inflammatory agent.

In vivo acute anti-inflammatory activity of the final compounds (9, 10 and 11) was evaluated in rat using egg-white induced edema model of inflammation in a dose equivalent to (7.5mg / Kg) of mefenamic acid.

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-amino-N-methylbenzenesulfonamide derivative (compound 10) exhibited comparable anti-inflammatory activity to diclofenac (3mg / Kg) at times 180-300 minute with the same onset of action.

The results of this study indicate that the incorporation of the 4-aminobenzenesulfonamide pharmacophore and its derivatives in to mefenamic acid maintain its anti-inflammatory activity.