Synthesis and preliminary pharmacological evaluation of aminobenzensulfonamides derivatives of diflunisal as a anti-inflammatory agents

الملخص EN

Objective : Synthesized of amino derivatives [٤-aminobenzenesulfonamide, ٤-amino-Nmethylbenzenesulfonamide, or N-(٤-aminophenylsulfonyl) acetamide] bound to carboxyl group of diflunisal, a well known nonsteroidal anti-inflammatory drugs (NSAIDs).

and evaluation as a potential anti-inflammatory agent with expected selectivity against COX-٢ enzyme.

Design : Expermental study Results : In vivo acute anti-inflammatory activity of the final compounds (١٣, ١٤ & ١٥) was evaluated in rat using egg-white induced edema model of inflammation in a dose equivalent to (٥٠mg / Kg) of diflunisal.

All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol ٥٠% v/v (control group).

Moreover, compound (١٤) exhibited comparable anti-inflammatory activity to diclofenac (٣mg / Kg), while compound (١٣) showed short duration of action, and compound (١٥) exhibited comparable effect to that of diclofenac with slower onset of action.

Conclusion : The result of this study indicate that the incorporation of the ٤-aminobenzenesulfonamide pharamacophore & its derivatives into diflunisal enhanced its anti-inflammatory activity& may increased its selectivity toward COX-٢ enzyme which can be confirmed in future by assessing COX- ٢:COX-١ inhibitory ratio using whole blood assay.