Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamidesAQ3 as carbonic anhydrase isoforms I and II inhibitors

Title
Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamidesAQ3 as carbonic anhydrase isoforms I and II inhibitors
Authors
이소하노은주백소라모하메드아메드실비아와디클라우디
Issue Date
2019-08
Publisher
Journal of enzyme inhibition and medicinal chemistry
Citation
VOL 34, NO 1-1464
Abstract
Carbonic anhydrases (CAs, EC 4.2.1.1) 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.
URI
http://pubs.kist.re.kr/handle/201004/70074
ISSN
1475-6366
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KIST Publication > Article
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