Browsing by Author "Evranos-Aksoz, Begum"
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Conference Object Citation - WoS: 0Design 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[Abstract Not Available]Conference Object Citation - WoS: 0Synthesis 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[Abstract Not Available]Article Citation - WoS: 49Citation - Scopus: 59Synthesis 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, RahmiyeA 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.