title: In vitro inhibition effect of some chalcones on erythrocyte carbonic anhydrase I and II.
abstract: In this study, 4'-(phenylurenyl/thiourenyl)chalcones (14-25) were prepared from 4'-(phenylurenyl/thiourenyl)acetophenones and benzaldehyde derivatives by Claisen-Schmidt condensation. In vitro inhibition effects of chalcone derivatives on purified carbonic anhydrase I and carbonic anhydrase II were investigated by using the CO2 hydration method of Maren. The result showed that all the synthesized compounds inhibited the CA isoenzymes activity. 18 and 19 were found to be most active (IC50 = 25.41 μM and 23.06 μM) for hCA I, respectively. For hCA II, 24 is the most active compound (IC50 = 14.40 μM).
authors: Department of Chemistry, Faculty of Art and Sciences, Balikesir University , Balikesir , Turkey.
authors: Nahit
authors: N
authors: Gençer
authors: Çiğdem
authors: Ç
authors: Bilen
authors: Dudu
authors: D
authors: Demir
authors: Alparslan
authors: A
authors: Atahan
authors: Mustafa
authors: M
authors: Ceylan
authors: Mustafa
authors: M
authors: Küçükislamoğlu
mesh_terms: D024401:Carbonic Anhydrase I / Q000037:antagonists & inhibitors; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors*; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D047188:Chalcones / Q000737:chemistry* / Q000494:pharmacology*; D004912:Erythrocytes / Q000201:enzymology*; D006801:Humans; D020128:Inhibitory Concentration 50; D010671:Phenylurea Compounds / Q000737:chemistry; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000737:chemistry
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D047188:Chalcones; D010671:Phenylurea Compounds; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II; D013890:Thiourea