biostudies-literatureUnknown37(1)Najm MAAthe Italian Ministry for University and ResearchThe 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</bJournal of enzyme inhibition and medicinal chemistry2702-2709https://www.ebi.ac.uk/biostudies/studies/S-EPMC9542353biostudies-literatureDesign and synthesis of some new benzoylthioureido phenyl derivatives targeting carbonic anhydrase enzymes.PMC9542353Taher ATAwadallah FMVullo DMahmoud WRNajm MAAAbbas SEAllam HASupuran CTfalseDesign and synthesis of some new benzoylthioureido phenyl derivatives targeting carbonic anhydrase enzymes.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</b2022-01-01T00:00:00Z2022 Dec2025-04-25T17:35:10.416Z2025-04-06T05:03:18.212ZS-EPMC95423533616812210.1080/14756366.2022.2126463