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Synthesis and Screening of Human Monoamine Oxidase-A Inhibitor Effect of New 2-Pyrazoline and Hydrazone Derivatives

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Synthesis and Screening of Human Monoamine Oxidase-AInhibitor Effect of New 2-Pyrazoline and Hydrazone Derivatives.pdf (1.230Mb)
Date
2015
Author
Evranos-Aksoz, Begüm
Baysal, İpek
Yabanoğlu-Çiftçi, Samiye
Djikic, Teodora
Yelekçi, Kemal
Uçar, Gülberk
Ertan, Rahmiye
Abstract
A group of 35-diaryl-2-pyrazoline and hydrazone derivatives was prepared via the reaction of various chalcones with hydrazide compounds in ethanol. Twenty original compounds were synthesized. Ten of these original compounds have a pyrazoline structure nine of these original compounds have a hydrazone structure and one of these original compounds has a chalcone structure. Structural elucidation of the compounds was performed by IR H-1 NMR C-13 NMR mass spectral data and elemental analyses. These compounds were tested for their inhibitory activities toward the A and B isoforms of human monoamine oxidase (MAO). Except for 3k and 6c all compounds were found to be competitive reversible and selective inhibitors for either one of the isoforms (hMAO-A or MAO-B). Compounds 3k and 6c were found to be competitive reversible but non-selective MAO inhibitors. Compound 6h showed hMAO-B inhibitory activity whereas the others potently inhibited hMAO-A. Compound 5c showed higher selectivity than the standard drug moclobemide. According to the experimental K-i values compounds 6i 6d and 6a exhibited the highest inhibitory activity toward hMAO-A. The AutoDock 4.2 program was employed to perform automated molecular docking. The calculated results obtained computationally were in good agreement with the experimental values.

Source

Archiv Der Pharmazie

Issue

10

Volume

348

Pages

743-756

URI

https://hdl.handle.net/20.500.12469/569
https://dx.doi.org/10.1002/ardp.201500212

Collections

  • Araştırma Çıktıları / PubMed [194]
  • Araştırma Çıktıları / Scopus [1565]
  • Araştırma Çıktıları / WOS [1518]
  • Biyoinformatik ve Genetik / Bioinformatics and Genetics [220]

Keywords

2-Pyrazoline
Hydrazone
MAO inhibitors
Molecular docking

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