Synthesis of new series of thiazol-(2(3H)-ylideneamino)benzenesulfonamide derivatives as carbonic anhydrase inhibitors.

Human carbonic anhydrase I and II isoenzymes (hCA I and II) are important metabolic enzymes. In this study, a new series of thiazol-(2(3H)-ylideneamino)benzenesulfonamide derivatives were synthesized and also some inhibition parameters including IC50 (hydratese) and inhibition constant values (Ki , esterase) were determined. All studied compounds exhibited potent inhibition against these enzymes. They inhibited carbonic anhydrases (CAs) with the IC50 values of 113 to 395.8 nM (Ki = 77.38-319.59 nM) for hCA I and 91.9 to 516 nM (Ki = 62.79-425.89 nM) for hCA II. Among the compounds, 5c was found to be the most active one (Ki : 77.38 nM) for hCA I and 5g was found for hCA II with the value of 62.79 nM.