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Browsing by Author "Evranos-Aksoz, Begum"

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    Design and Synthesis of Novel 2-Pyrazoline Analogues and Their Hmao Inhibitory Activities
    (Wiley-Blackwell, 2015) Uçar, Gülberk; Yelekçi, Kemal; Evranos-Aksoz, Begum; Yabanoglu-Çiftçi, Samiye; Yelekçi, Kemal; Molecular Biology and Genetics
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    Synthesis and Screening of Hmao Inhibitory Activities of Some New 2-Pyrazoline and Hydrazone Derivatives
    (Wiley-Blackwell, 2014) Evranos-Aksoz, Begum; Yelekçi, Kemal; Yabanoglu-Ciftci, Samiye; Ucar, Gulberk; Yelekçi, Kemal; Ertan, Rahmiye; Molecular Biology and Genetics
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    Synthesis of Some Novel Hydrazone and 2-Pyrazoline Derivatives: Monoamine Oxidase Inhibitory Activities and Docking Studies
    (Pergamon-Elsevier Science Ltd, 2014) Evranos-Aksoz, Begum; Yelekçi, Kemal; Yabanoglu-Ciftci, Samiye; Ucar, Gulberk; Yelekçi, Kemal; Ertan, Rahmiye; Molecular Biology and Genetics
    A novel series of 2-pyrazoline and hydrazone derivatives were synthesized and investigated for their human monoamine oxidase (hMAO) inhibitory activity. All compounds inhibited the hMAO isoforms (MAO-A or MAO-B) competitively and reversibly. With the exception of 5i which was a selective MAO-B inhibitor all derivatives inhibited hMAO-A potently and selectively. According to the experimental K-i values compounds 6e and 6h exhibited the highest inhibitory activity towards the hMAO-A whereas compound 5j which carries a bromine atom at R-4 of the A ring of the pyrazoline appeared to be the most selective MAO-A inhibitor. Tested compounds were docked computationally into the active site of the hMAO-A and hMAO-B isozymes. The computationally obtained results were in good agreement with the corresponding experimental values. (C) 2014 Elsevier Ltd. All rights reserved.