Benzamide sulfonamide derivatives: potent inhibitors of carbonic anhydrase-II

Abstract

Benzamide sulfonamide and its derivatives were identified as potent inhibitors of carbonic anhydrase-II (bovine carbonic anhydrase-II (bCA-II) and human recombinant carbonic anhydrase-II (hCA-II)) with IC50 values 0.06–0.28 μM and 0.09–0.58 μM, respectively. Different kinetics parameter, such as Vmax, Km, and Ki, were determined. Molecular docking simulation studies on the lead compounds were carried out by AutoDock Vina docking software. The compounds were also evaluated for their cytotoxicity against 3T3 (Normal Cell Lines Mouse Fibroblast) cell line. All the compounds have shown non-cytotoxic effect toward 3T3 cell lines. This study has identified novel scaffolds for further hit-to-lead optimization for the discovery of effective drugs against carbonic anhydrase-II-associated disorder, such as glaucoma, leukemia, cystic fibrosis, and epilepsy.