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  • [ X ]
    Öğe
    Synthesis of new series of thiazol-(2(3H)-ylideneamino)benzenesulfonamide derivatives as carbonic anhydrase inhibitors
    (Wiley, 2020) Berber, Nurcan; Arslan, Mustafa; Vural, Firat; Ergun, Adem; Gencer, Nahit; Arslan, Oktay
    Human carbonic anhydrase I and II isoenzymes (hCA I and II) are important metabolic enzymes. In this study, a new series of thiazol-(2(3H)-ylideneamino)benzenesulfonamide derivatives were synthesized and also some inhibition parameters including IC50(hydratese) and inhibition constant values (K-i, esterase) were determined. All studied compounds exhibited potent inhibition against these enzymes. They inhibited carbonic anhydrases (CAs) with the IC(50)values of 113 to 395.8 nM (K-i = 77.38-319.59 nM) for hCA I and 91.9 to 516 nM (K-i = 62.79-425.89 nM) for hCA II. Among the compounds,5cwas found to be the most active one (K-i: 77.38 nM) for hCA I and5gwas found for hCA II with the value of 62.79 nM.
  • [ X ]
    Öğe
    Synthesis, characterization, carbonic anhydrase inhibitor activity, and docking studies of phenylthiazol-2 (3h)-ylidene-isoquinoline-5-amine Derivatives
    (Elsevier, 2023) Berber, Nurcan; Sahutoglu, Arif Sercan; Gokce, Basak; Cikrikci, Kuebra; Gencer, Nahit
    Phenylthiazol-2(3h)-ylidene-isoquinoline-5-amine derivatives(5a-r) were easily prepared from 5-aminoisoquinoline, thioisocyanate, and phenacyl bromide derivatives in the presence of triethylamine in tetrahydrofuran (THF), and dimethyl formamide (DMF) in two steps. In the first step, thiourea was synthesized in THF reflux, 24 h and then in the second step, the formation of thiazole ring was ensured in EtOH-DMF (5:5 v/v), reflux, 24 h. The newly synthesized compounds were characterized using 1H NMR, 13C NMR, IR, and elemental analysis. The inhibitory effects of 18 newly synthesized compounds (5a-r) on hydratase and esterase activities of carbonic anhydrase isoenzymes (hCA I, II, IX, and X) were studied in vitro.