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Öğe In vitro inhibition of purified human carbonic anhydrase I and II by novel fluorene derivatives(Macedonian Journal of Chemistry and Chemical Engineering, 2014) Demirhan, Hulya; Arslan, Mustafa; Kaya, Mustafa Oguzhan; Kaya, Yesim; Gencer, Nahit; Arslan, OktayIn this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 ?M) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 ?M) for inhibition of hCA II.Öğe IN VITRO INHIBITION OF PURIFIED HUMAN CARBONIC ANHYDRASE I AND II BY NOVEL FLUORENE DERIVATIVES(Soc Chemists Technologists Madeconia, 2014) Demirhan, Hulya; Arslan, Mustafa; Kaya, Mustafa Oguzhan; Kaya, Yesim; Gencer, Nahit; Arslan, OktayIn this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 mu M) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 mu M) for inhibition of hCA II.Öğe Synthesis and carbonic anhydrase inhibitory properties of tetrazole- and oxadiazole substituted 1,4-dihydropyrimidinone compounds(Informa Healthcare, 2014) Celik, Fatma; Arslan, Mustafa; Kaya, Mustafa Oguzhan; Yavuz, Emre; Gencer, Nahit; Arslan, OktayA new series of tetrazole-, oxadiazole-and cyanosubstituted 1,4-dihydropyrimidinone compounds were synthesized, and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I were evaluated. 4-Cyanophenyl-1,4- dihydropyrimidinone compounds were prepared with 1,3-diketone, cyanobenzaldehyde and urea. The compounds were reacted with sodium azide and then with anhydride to get the final products. The results showed that all the synthesized compounds inhibited the CA isoenzyme activity. The compound 4-(1,7,7-trimethyl-2,5-dioxo-1,2,3,4,5,6,7,8-octahydroquinazoline- 4-yl) benzonitrile 6c (IC50 = 0.0547 mM) has the most inhibitory effect.