期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 37, 期 1, 页码 2702-2709出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2022.2126463
关键词
Sulphonamides; carbonic anhydrase; SLC-0111; benzoylthioureido derivatives
资金
- Italian Ministry for University and Research (MIUR) [FISR2019_04819 BacCAD]
This study aimed to develop potent carbonic anhydrase inhibitors (CAIs) by modifying the structure of a known inhibitor. Different compounds with substituted benzoylthioureido core and various zinc-binding groups were prepared and tested for their inhibitory activity against human CA isoforms. Some compounds showed significant inhibitory activity against a specific isoform, indicating their potential as promising drug candidates for glaucoma treatment.
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.
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