NO-releasing esters show carbonic anhydrase inhibitory action against human isoforms I and II.
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 IC(50) values of compounds 1-12 against hCA I ranged between 7.13mM and 124mM, and against hCA II between 65.1microM and 0.79mM. 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.
Ekinci
Deniz
D
Atatürk University, Science Faculty, Department of Chemistry, 25240 Erzurum, Turkey. dekinci80@gmail.com
Cavdar
Hüseyin
H
Talaz
Oktay
O
Sentürk
Murat
M
Supuran
Claudiu T
CT
D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors*; D002257:Carbonic Anhydrase Inhibitors / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000187:drug effects*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000494:pharmacology; D004912:Erythrocytes / Q000166:cytology / Q000187:drug effects; D004952:Esters / Q000737:chemistry*; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D008297:Male; D008954:Models, Biological; D009569:Nitric Oxide / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D002257:Carbonic Anhydrase Inhibitors; D004791:Enzyme Inhibitors; D004952:Esters; D007527:Isoenzymes; D009569:Nitric Oxide; D024402:Carbonic Anhydrase II; D002256:Carbonic Anhydrases