Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 10, Pages 3559-3563Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.03.082
Keywords
Organic nitrates; Carbonic anhydrase; Inhibition; hCA I; hCA II; Antiglaucoma
Funding
- European Union
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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 mu M 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. (C) 2010 Elsevier Ltd. All rights reserved.
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