(3, 4-Dihydroxyphenyl)(2, 3, 4-trihydroxyphenyl)methanone and its derivatives as carbonic anhydrase isoenzymes inhibitors. (April 2013)

• Record Type: Journal Article
• Authors: Nar, Meryem; Çetinkaya, Yasin; Gülçin, İlhami; Menzek, Abdullah
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 28:Number 2(2013:Apr.)
• Page Start: 402
• Page End: 406
• Publication Date: 2013-04
• Subjects: Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2012.670807
• Languages: English
• ISSNs: 1475-6366

Abstract

<abstract> <title> <x xml:space="preserve">Abstract</x> </title> <p>In this study, we have synthesised (3, 4-dihydroxyphenyl)(2, 3, 4-trihydroxyphenyl)methanone and a series of its derivatives (<bold>5</bold>, <bold>13–16</bold>) 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 (<bold>5, 13–16</bold>) 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 <bold>14</bold> showed the highest inhibiton effect against hCA I (IC₅₀: 3.22 μM; K_i: 1.19 ± 1.4 μM). On the other hand, the compound <bold>13</bold> showed the highest inhibiton effect against hCA II (IC₅₀: 18.52 μM; K_i: 3.25 ± 1.13 μM).</p> </abstract>