Meryem Nar, Yasin Çetinkaya, I. Gülçin
Feb 5, 2013
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Journal
Journal of Enzyme Inhibition and Medicinal Chemistry
Abstract
In this study, we have synthesised (3,4-dihydroxyphenyl)(2,3,4-trihydroxyphenyl)methanone and a series of its derivatives (5, 13–16) and tested the ability of these compounds to inhibit two metalloenzyme human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes, hCA I and hCA II. The synthesised compounds showed inhibitory effect on hCA I and hCA II isozymes. The results showed that synthesised compounds (5, 13–16) demonstrated the best inhibition activity against hCA I (IC50: 3.22–54.28 μM) and hCA II (IC50: 18.52–142.01 μM). The compound 14 showed the highest inhibiton effect against hCA I (IC50: 3.22 μM; Ki: 1.19 ± 1.4 μM). On the other hand, the compound 13 showed the highest inhibiton effect against hCA II (IC50: 18.52 μM; Ki: 3.25 ± 1.13 μM).