NO-releasing esters show carbonic anhydrase inhibitory action against human isoforms I and II

Ekinci D., Çavdar H., Talaz O., Şentürk M., Supuran C. T.

Bioorganic and Medicinal Chemistry, cilt.18, sa.10, ss.3559-3563, 2010 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 18 Sayı: 10
  • Basım Tarihi: 2010
  • Doi Numarası: 10.1016/j.bmc.2010.03.082
  • Dergi Adı: Bioorganic and Medicinal Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.3559-3563
  • Anahtar Kelimeler: Antiglaucoma, Carbonic anhydrase, hCA I, hCA II, Inhibition, Organic nitrates
  • Ondokuz Mayıs Üniversitesi Adresli: Evet

Özet

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. © 2010 Elsevier Ltd. All rights reserved.