Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamidesAQ3 as carbonic anhydrase isoforms I and II inhibitors
- Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamidesAQ3 as carbonic anhydrase isoforms I and II inhibitors
- 이소하; 노은주; 백소라; 모하메드; 아메드; 실비아; 와디; 클라우디
- Issue Date
- Journal of enzyme inhibition and medicinal chemistry
- VOL 34, NO 1-1464
- Carbonic anhydrases (CAs, EC 18.104.22.168) are crucial metalloenzymes that are involved in diverse bioprocesses. We report the synthesis and biological evaluation of novel series of benzenesulfonamides incorporating un/substituted ethyl quinoline-3-carboxylate moieties. The newly synthesised compounds were in vitro evaluated as inhibitors of the cytosolic human (h) isoforms hCA I and II. Both isoforms hCA I and II were inhibited by the quinolines reported here in variable degrees: hCA I was inhibited with KIs in the range of 0.966– 9.091 lM, whereas hCA II in the range of 0.083– 3.594 lM. The primary 7-chloro-6-flouro substituted sulphfonamide derivative 6e (KI ¼ 0.083 lM) proved to be the most active quinoline in inhibiting hCA II,
whereas, its secondary sulfonamide analog failed to inhibit the hCA II up to 10 lM, confirming the crucial role of the primary sulphfonamide group, as a zinc-binding group for CA inhibitory activity.
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