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An Insight into Synthetic and Docking Approaches of Benzenesulfonamide Scaffold Revealing COX-2 Inhibitors

[ Vol. 11 , Issue. 2 ]


Sandip D. Firake and Sanjaykumar B. Bari   Pages 76 - 107 ( 32 )


Benzenesulfonamide is versatile motif employed for the discovery in the field of medicinal and pharmaceutical chemistry. Over the years of active research, sulfonamide has evolved as important privileged pharmacophore in medicinal chemistry, encompassing a diverse range of biological activities including antiviral, carbonic anhydrase inhibitors, diuretic, and a protease inhibitor, hypoglycemic, anticancer and anti-inflammatory. On the other hand, owing to the fast development of new drugs possessing sulfonamide pharmacophore many research reports generated in a short span of time. Thus, there is a need to couple the most recent data with the prior data to comprehend the present status of benzenesulfonamide as anti-inflammatory agent. The present review highlights the molecular modeling and synthetic methods of benzenesulfonamide scaffold bearing various heterocyclic or carbocyclic rings such as thiazole, triazole, imidazole, isoxazoline, pyridine, pyranone, pyridazone, pyrimidine, pyran, indole, benzothiazole, benzotriazole, benzimidazole and benzopyran as central ring scaffold. In addition to this, the manuscript will be a guideline to medicinal chemists for rationally designing a novel benzenesulfonamide bearing compounds as COX-2 inhibitors.


Anti-inflammatory, benzenesulfonamide, COX-2, molecular modeling, pyrazole, synthesis.


Department of Pharmaceutical Chemistry, R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur-425405, MS, India.

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