Inhibition of human carbonic anhydrase isozymes I, II and VI with a series of bisphenol, methoxy and bromophenol compounds


Balaydin H. T. , Durdagi S., Ekinci D., Senturk M., GÖKSU S., MENZEK A.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.27, no.4, pp.467-475, 2012 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 27 Issue: 4
  • Publication Date: 2012
  • Doi Number: 10.3109/14756366.2011.596836
  • Title of Journal : JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Page Numbers: pp.467-475
  • Keywords: Carbonic anhydrase, molecular docking, bisphenol, bromophenol, hCA II, hCA VI, ERYTHROCYTE GLUTATHIONE-REDUCTASE, THERAPEUTIC APPLICATIONS, VITRO INHIBITION, METAL-COMPLEXES, SULFONAMIDES, PURIFICATION, THIOXOLONE, DRUGS

Abstract

Carbonic anhydrase inhibitors (CAI) are valuable molecules as they have several therapeutic applications, including anti-glaucoma activity. In this study, inhibition of three human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I, II and VI with a series of bisphenol and bromophenol derivatives was investigated. Molecular docking studies of a set of such inhibitors within CA I and II were also performed. K-I values of the molecules 2-9 were in the range of 10.025-892.109 mu M for hCA I, 1.437-59.107 mu M for hCA II and 11.143-919.182 mu M for hCA VI, respectively. Reported inhibitory activities of molecules 2-9 will assist in better understanding of structure-activity relationship studies of CAI.