Synthesis and carbonic anhydrase inhibitory properties of novel chalcone substituted benzenesulfonamides

Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes involved in many bioprocesses, through catalysis of the reversible hydration/dehydration process of CO2/HCO3-. The inhibition of human CA isoforms I and II with a new series of sulfonamide derivatives incorporating substituted chalcone moieties were studied in this study. All these newly synthesized sulfonamides demonstrated important inhibitory profiles to these CA isoforms with K(1)s in the range of 9.88 to 55.43 nM, making these compounds interesting leads, with potential applications in medicinal chemistry. (C) 2016 Published by Elsevier Ltd.