Synthesis of some novel hydrazone and 2-pyrazoline derivatives: Monoamine oxidase inhibitory activities and docking studies

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Date

2014

Authors

Yabanoglu-Ciftci, Samiye
Ucar, Gulberk
Yelekçi, Kemal
Ertan, Rahmiye

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Publisher

Pergamon-Elsevier Science Ltd

Research Projects

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Abstract

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.

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Keywords

2-Pyrazoline, Hydrazone, MAO inhibitors, Molecular docking

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Citation

47

WoS Q

N/A

Scopus Q

Q2

Source

Volume

24

Issue

15

Start Page

3278

End Page

3284