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Abstract #105884 Published in IGR 23-3
Design and synthesis of some new benzoylthioureido phenyl derivatives targeting carbonic anhydrase enzymes
Najm MAA; Mahmoud WR; Taher AT; Abbas SE; Awadallah FM; Allam HA; Vullo D; Supuran CTJournal of Enzyme Inhibition and Medicinal Chemistry 2022; 37: 2702-2709
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 and , its bioisosteric carboxylic acid group and or the ethyl carboxylate group and 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 , , , , and revealed significant inhibitory activity against hCA I that would highlight these compounds as promising drug candidates for the treatment of glaucoma.
Department of Pharmaceutical Chemistry, College of Pharmacy, Al-Ayen University, Thi-Qar, Iraq.
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