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    A novel proton transfer salt of 2-amino-6-sulfamoylbenzothiazole and its metal complexes: the evaluation of their inhibition effects on human cytosolic carbonic anhydrases
    (Taylor & Francis Ltd, 2017) Alkaya, Zeynep Alkan; İlkimen, Halil; Yenikaya, Cengiz; Kaygısız, Yasemin; Bülbül, Metin; Tunç, Tuncay; Sarı, Musa
    A novel proton transfer compound (SMHABT) (+)(HDPC)(-) (1) obtained from 2-amino-6-sulfamoylbenzothiazole (SMABT) and 2,6-pyridinedicarboxylic acid (H2DPC) and its Fe(III), Co(II), Ni(II) complexes (2-4), and Fe(II) complex of SMABT (5) have been prepared and characterized by spectroscopic techniques. Additionally, single crystal X-ray diffraction techniques were applied to complexes (2-4). All complexes (2-4) have distorted octahedral conformations and the structure of 5 might be proposed as octahedral according to spectral and analytical results. All compounds, including acetazolamide (AAZ) as the control compound, were also evaluated for their in vitro inhibition effects on human hCA I and hCA II for their hydratase and esterase activities. The synthesized compounds have remarkable inhibitory activities on hCA I and hCA II. Especially, the inhibition potentials of the salt and the metal complexes (1-5) are comparable with AAZ. Inhibition data have been analyzed by using a one-way analysis of variance for multiple comparisons (p < .0001).
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    Synthesis and characterization of Cu(II) complexes of 2-amino-6-sulfamoylbenzothiazole and their inhibition studies on carbonic anhydrase isoenzymes
    (Pergamon-Elsevier Science Ltd, 2018) Alkan Alkaya, Zeynep; İlkimen, Halil; Yenikaya, Cengiz; Tunca, Ekrem; Bülbül, Metin; Tunç, Tuncay; Sarı, Musa
    2-Amino-6-sulfamoylbenzothiazole (SMABT) and its proton transfer compound (HSMABT)(+)(HDPC)(-) (1) with 2,6-pyridinedicarboxylic acid (H2DPC), and their Cu(II) complexes (2 of SMABT, 3 and 4 of 1) have been prepared and characterized by spectroscopic techniques. Additionally, single crystal X-ray diffraction techniques were applied to all complexes. All compounds, including acetazolamide (AAZ) as the control compound, were also evaluated for their in vitro inhibition effects on human hCA I and hCA II for their hydratase and esterase activities. The synthesized complexes have remarkable inhibitory effects on hCA I and hCA II isoenzymes. The inhibition potentials of the proton transfer salt (1) and the metal complexes (2-4) are comparable with AAZ. Esterase K-i values of the compounds (1-4) are in the range of 0.089 +/- 0.008 mu M-0.149 +/- 0.017 mu M for hCA I and 0.046 +/- 0.008 mu M-0.085 +/- 0.019 mu M for hCA II. Inhibition data have been analyzed by using a one-way analysis of variance for multiple comparisons (p < 0.0001). (C) 2018 Published by Elsevier Ltd.
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    Synthesis, characterization, and pharmacological evaluation of the proton transfer salts of 2-aminobenzothiazole derivatives with 5-sulfosalicylic acid and their Cu(II) complexes
    (Taylor & Francis, 2018) İlkimen, Halil; Teksen, Yasemin; Yenikaya, Cengiz; Turhan, Irem; Tunç, Tuncay; Sarı, Musa
    Two proton transfer compounds, formed between 2-aminobenzothiazole derivatives (2-aminobenzothiazole (abt) and 2-amino-6-ethoxybenzothiazole (EtOabt)) and 5-sulfosalicylic acid dihydrate (H3ssa) as parent compounds, (Habt)(+) (H2ssa)(-) (1) and (HEtOabt)(+) (H2ssa)(-) (2) and their Cu(II) complexes (3 and 4, respectively) have been prepared and characterized using spectroscopic techniques. The single crystal X-ray diffraction method has been also applied to 3 and 4. Although 3 has a distorted octahedral form, 4 exhibits a distorted square pyramidal geometry. All compounds, including saline and diclofenac sodium as standards, have been evaluated pharmacologically for their anti-inflammatory and analgesic activities in rats and mice. Parent compounds (abt, EtOabt, and H3ssa) 3 and 4 showsignificant anti-inflammatory and analgesic activities as compared with control compounds. [GRAPHICS] .