Sulfonamide derivatives with benzothiazole scaffold: Synthesis and carbonic anhydrase I –II inhibition properties

AbstractThe secondary sulfonamide derivatives containing benzothiazole scaffold (1 –10) were synthesized to determine their inhibition properties on two physiologically essential human carbonic anhydrases isoforms (hCAs, EC, 4.2.1.1), hCA I, and hCA II. The inhibitory effects of the compounds on hCA I and hCA II isoenzymes were investigated by comparing their IC50 andKi values. TheKi values of compounds (1 –10) against hCA I and hCA II are in the range of 0.052  ± 0.022–0.971 ± 0.280 and 0.025 ± 0.010–0.682 ± 0.335, respectively. Some of these inhibited the enzyme more effectively than the standard drug, acetazolamide. In particular, compounds5 and4 were found to be most effective on hCA I and hCA II.

Source: Biotechnology and Applied Biochemistry - November 15, 2023 Category: Biochemistry Authors: Cansu Öztürk, Erbay Kalay, Serpil Gerni, Neslihan Balci, Feyzi Sinan Tokali, Osman Nuri Aslan, Emrah Polat Tags: ORIGINAL ARTICLE Source Type: research