Design 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 revealed significant inhibitory activity against hCA I that would highlight these compounds as promising drug candidates for the treatment of glaucoma.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:37 |
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| Enthalten in: |
Journal of enzyme inhibition and medicinal chemistry - 37(2022), 1 vom: 27. Dez., Seite 2702-2709 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Najm, Mazin A A [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 29.09.2022 Date Revised 11.10.2022 published: Print Citation Status MEDLINE |
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| doi: |
10.1080/14756366.2022.2126463 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM346837278 |
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| 245 | 1 | 0 | |a Design and synthesis of some new benzoylthioureido phenyl derivatives targeting carbonic anhydrase enzymes |
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| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a SLC-0111 | |
| 650 | 4 | |a Sulphonamides | |
| 650 | 4 | |a benzoylthioureido derivatives | |
| 650 | 4 | |a carbonic anhydrase | |
| 650 | 7 | |a Carbonic Anhydrase Inhibitors |2 NLM | |
| 650 | 7 | |a Carboxylic Acids |2 NLM | |
| 650 | 7 | |a Prodrugs |2 NLM | |
| 650 | 7 | |a Carbonic Anhydrase IX |2 NLM | |
| 650 | 7 | |a EC 4.2.1.1 |2 NLM | |
| 650 | 7 | |a Carbonic Anhydrases |2 NLM | |
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| 650 | 7 | |a Zinc |2 NLM | |
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| 700 | 1 | |a Mahmoud, Walaa R |e verfasserin |4 aut | |
| 700 | 1 | |a Taher, Azza T |e verfasserin |4 aut | |
| 700 | 1 | |a Abbas, Safinaz E-S |e verfasserin |4 aut | |
| 700 | 1 | |a Awadallah, Fadi M |e verfasserin |4 aut | |
| 700 | 1 | |a Allam, Heba Abdelrasheed |e verfasserin |4 aut | |
| 700 | 1 | |a Vullo, Daniela |e verfasserin |4 aut | |
| 700 | 1 | |a Supuran, Claudiu T |e verfasserin |4 aut | |
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