title: (3,4-Dihydroxyphenyl)(2,3,4-trihydroxyphenyl)methanone and its derivatives as carbonic anhydrase isoenzymes inhibitors.
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 (IC(50): 3.22-54.28 μM) and hCA II (IC(50): 18.52-142.01 μM). The compound 14 showed the highest inhibiton effect against hCA I (IC(50): 3.22 μM; K(i): 1.19 ± 1.4 μM). On the other hand, the compound 13 showed the highest inhibiton effect against hCA II (IC(50): 18.52 μM; K(i): 3.25 ± 1.13 μM).
authors.affiliation: Department of Chemistry, Faculty of Sciences, Atatürk University, Erzurum, Turkey.
authors.forename: Meryem
authors.initials: M
authors.lastname: Nar
authors.forename: Yasin
authors.initials: Y
authors.lastname: Çetinkaya
authors.forename: İlhami
authors.initials: İ
authors.lastname: Gülçin
authors.forename: Abdullah
authors.initials: A
authors.lastname: Menzek
mesh_terms: D001577:Benzophenones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002245:Carbon Dioxide / Q000737:chemistry / Q000378:metabolism; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D015394:Molecular Structure; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001577:Benzophenones; D002257:Carbonic Anhydrase Inhibitors; D020033:Protein Isoforms; D002245:Carbon Dioxide; D002256:Carbonic Anhydrases