NO-releasing esters show carbonic anhydrase inhibitory action against human isoforms I and II |
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| Authors: | Deniz Ekinci Hüseyin Çavdar Oktay Talaz Murat Şentürk Claudiu T. Supuran |
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| Affiliation: | 1. Atatürk University, Science Faculty, Department of Chemistry, 25240 Erzurum, Turkey;2. Dumlup?nar University, Education Faculty, 43100 Kütahya, Turkey;3. A?r? ?brahim Çeçen University, Art and Science Faculty, Department of Chemistry, 04100 A?r?, Turkey;4. Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy |
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| Abstract: | Carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) are a class of pharmaceuticals used as antiglaucoma agents, diuretics, antiepileptics, in the management of mountain sickness, gastric and duodenal ulcers, neurological disorders, or osteoporosis. We report here the inhibitory capacities of some organic nitrates against two human (hCA) isozymes, hCA I and hCA II. The IC50 values of compounds 1–12 against hCA I ranged between 7.13 mM and 124 mM, and against hCA II between 65.1 μM and 0.79 mM. Nitrate esters are thus interesting hCA I and II inhibitors, and might be used as leads for generating enzyme inhibitors eventually targeting other isoforms which have not been assayed yet for their interactions with such agents. |
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