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

OpenAlex İngilizce

Abstract 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.