Synthesis and Preliminary Pharmacological Evaluation of Aminobenzensulfonamides Derivatives of Mefenamic Acid as a Potential Anti-inflammatory Agents

• Main Author: Monther F. Mahdi (Author)
• Format: Book
• Published: College of Pharmacy University of Baghdad, 2017-03-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 2521-3512; 1683-3597
• Keywords: Pharmacy and materia medica; RS1-441
• Source: Iraqi Journal of Pharmaceutical Sciences, Vol 17, Iss 1 (2017)

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. Key ward: benzenesulfonamide, anti-inflammatory, paw edema, NSAIDs, mefenamic acid