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    Microwave-assisted synthesis of 1-substituted-1H-benzimidazolium salts: Non-competitive inhibition of human carbonic anhydrase I and II
    (Wiley-V C H Verlag Gmbh, 2019) Karlik, Ozgul; Gencer, Nahit; Karatas, Mert O.; Ergun, Adem; Cikrikci, Kubra; Arslan, Oktay; Alici, Bulent
    A series of 1-substituted-1H-benzimidazolium p-toluenesulfonate salts were synthesized in good yields by the reaction of 1-substituted benzimidazole derivatives and p-toluenesulfonic acid under microwave irradiation. Two iodide salts were synthesized by the anion exchange reaction of the corresponding p-toluenesulfonate salt and NaI. All compounds were characterized by H-1 NMR, C-13 NMR, IR, LC-MS spectroscopic methods, and elemental analyses. The crystal structure of 1-methoxyethyl-1H-benzimidazolium p-toluenesulfonate 2d showed that cation and anion are interconnected by N-H center dot center dot center dot O and C-H center dot center dot center dot O hydrogen bonds. All compounds were examined as inhibitor of human carbonic anhydrase (hCA) I and II, and all of them inhibited hCA I and hCA II. Kinetic investigation results revealed that these compounds inhibit hCA I and hCA II in a non-competitive manner. The iodide salts had higher inhibitory activity than their corresponding p-toluenesulfonate salts.
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    New coumarin derivatives as carbonic anhydrase inhibitors
    (Taylor & Francis Ltd, 2014) Karatas, Mert Olgun; Alici, Bulent; Cakir, Umit; Cetinkaya, Engin; Demir, Dudu; Ergun, Adem; Gencer, Nahit
    In the current study, a series of 4-chloromethyl-7-hydroxy-coumarin derivatives containing imidazolium, benzimidazolium, bisbenzimidazolium and quaternary ammonium salts were synthesized, characterized and the inhibition effects of the derivatives on human carbonic anhydrases (hCA I and hCA II) were investigated as in vitro. Structures of these coumarins were confirmed by FT-IR, (1)H NMR, (13)C NMR and LC-MS analyses. Structure activity relationship study showed that 3d (IC50: 79 mu m M for hCA I and 88 m M for hCA II) performed higher inhibitory activity than others.
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    Synthesis and carbonic anhydrase inhibitory properties of novel coumarin derivatives
    (Informa Healthcare, 2013) Karatas, Mert Olgun; Alici, Bulent; Cakir, Umit; Cetinkaya, Engin; Demir, Dudu; Ergun, Adem; Gencer, Nahit
    A newly series of water-soluble 1-alkyl-3-(4-methyl-7, 8-dihydroxy-2H-chromen-2-one) benzimidazolium chloride salts (3a-j) were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II from human erythrocytes were purified by a simple one step procedure by using Sepharose 4B-L-tyrosine-sulphanilamide affinity column. The result showed that all the synthesized compounds were inhibited the CA isoenzymes activity. Among them, 3g and 3j were found to be most active (IC50 = 22.09 mu M and 20.33 mu M) for hCA I and hCA II, respectively.