%0 Journal Article
%T Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamides as carbonic anhydrase isoforms I and II inhibitors
%A Ahmed Elkamhawy
%A Claudiu T. Supuran
%A Eun Joo Roh
%A Mohamed A. Abdelgawad
%A Silvia Bua
%A So Ha Lee
%A Sora Paik
%A Wagdy M. Eldehna
%J Journal of Enzyme Inhibition and Medicinal Chemistry
%D 2019
%R https://doi.org/10.1080/14756366.2019.1652282
%X 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¨C9.091£¿¦ÌM, whereas hCA II in the range of 0.083¨C3.594£¿¦ÌM. The primary 7-chloro-6-flouro substituted sulphfonamide derivative 6e (KI = 0.083£¿¦ÌM) 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£¿¦ÌM, confirming the crucial role of the primary sulphfonamide group, as a zinc-binding group for CA inhibitory activity
%U https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1652282