期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 27, 期 4, 页码 467-475出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2011.596836
关键词
Carbonic anhydrase; molecular docking; bisphenol; bromophenol; hCA II; hCA VI
资金
- Turkish Republic Prime Ministry State Planning Organization (DPT) [2010K120440]
- Agri Ibrahim Cecen University Scientific Research Council [Agri BAP-2010/K-10]
- Scientific and Technological Research Council of Turkey (TUBITAK) [TBAG-107T/348]
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.
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