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.
NO-releasing esters show carbonic anhydrase inhibitory action against human isoforms I and II / D. Ekinci;H. Cavdar;O. Talaz;M. Sentürk;C. T. Supuran. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 18:(2010), pp. 3559-3563. [10.1016/j.bmc.2010.03.082]
NO-releasing esters show carbonic anhydrase inhibitory action against human isoforms I and II.
SUPURAN, CLAUDIU TRANDAFIR
2010
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 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.
I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
