The present study aimed to develop potent carbonic anhydrase inhibitors (CAIs). The design of the target compounds was based on modifying the structure of the ureido-based carbonic anhydrase inhibitor SLC-0111. Six series of a substituted benzoylthioureido core were prepared featuring different zinc-binding groups; the conventional sulphamoyl group 4a-d and 12a-c, its bioisosteric carboxylic acid group 5a-d and 13a-c or the ethyl carboxylate group 6a-d and 14a-c as potential prodrugs. All compounds were assessed for their carbonic anhydrase (CA) inhibitory activity against a panel of four physiologically relevant human CA isoforms hCA I and hCA II, and hCA IX, and hCA XII. Compounds 4a, 4b, 4c, 4d, 5d, 12a, and 12c revealed significant inhibitory activity against hCA I that would highlight these compounds as promising drug candidates for the treatment of glaucoma.

Design and synthesis of some new benzoylthioureido phenyl derivatives targeting carbonic anhydrase enzymes / Najm, Mazin A A; Mahmoud, Walaa R; Taher, Azza T; Abbas, Safinaz E-S; Awadallah, Fadi M; Allam, Heba Abdelrasheed; Vullo, Daniela; Supuran, Claudiu T. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - ELETTRONICO. - 37:(2022), pp. 0-0. [10.1080/14756366.2022.2126463]

Design and synthesis of some new benzoylthioureido phenyl derivatives targeting carbonic anhydrase enzymes

Vullo, Daniela;Supuran, Claudiu T
2022

Abstract

The present study aimed to develop potent carbonic anhydrase inhibitors (CAIs). The design of the target compounds was based on modifying the structure of the ureido-based carbonic anhydrase inhibitor SLC-0111. Six series of a substituted benzoylthioureido core were prepared featuring different zinc-binding groups; the conventional sulphamoyl group 4a-d and 12a-c, its bioisosteric carboxylic acid group 5a-d and 13a-c or the ethyl carboxylate group 6a-d and 14a-c as potential prodrugs. All compounds were assessed for their carbonic anhydrase (CA) inhibitory activity against a panel of four physiologically relevant human CA isoforms hCA I and hCA II, and hCA IX, and hCA XII. Compounds 4a, 4b, 4c, 4d, 5d, 12a, and 12c revealed significant inhibitory activity against hCA I that would highlight these compounds as promising drug candidates for the treatment of glaucoma.
2022
37
0
0
Najm, Mazin A A; Mahmoud, Walaa R; Taher, Azza T; Abbas, Safinaz E-S; Awadallah, Fadi M; Allam, Heba Abdelrasheed; Vullo, Daniela; Supuran, Claudiu T
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1306064
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