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01-06-2013 | Translational Neurosciences - Original Article

Evaluation of selective human MAO inhibitory activities of some novel pyrazoline derivatives

Authors: Umut Salgın-Gökşen, Samiye Yabanoğlu-Çiftçi, Ayşe Ercan, Kemal Yelekçi, Gülberk Uçar, Nesrin Gökhan-Kelekçi

Published in: Journal of Neural Transmission | Issue 6/2013

Abstract

A series of 1-[2-((5-methyl/chloro)-2-benzoxazolinone-3-yl)acetyl]-3,5-diaryl-4,5-dihydro-1H-pyrazole derivatives were prepared by reacting 2-((5-methyl/chloro)-2-benzoxazolinone-3-yl)acetylhydrazine with appropriate chalcones. The chemical structures of all compounds were confirmed by elemental analyses, IR, ¹H NMR and ESI–MS. All the compounds were investigated for their ability to selectively inhibit monoamine oxidase (MAO) by in vitro tests. MAO activities of the compounds were compared with moclobemide and selegiline and all the compounds were found to inhibit human MAO-A selectively. The inhibition profile was found to be competitive and reversible for all compounds by in vitro tests. Among the compounds examined, compounds 5ae, 5af and 5ag were more selective than moclobemide, with respect to the K _i values experimentally found. In addition, the compound 5bg showed MAO-A inhibitor activity as well as moclobemide. A series of experimentally tested compounds (5ae–5ch) were docked computationally to the active site of the MAO-A and MAO-B isoenzyme. The AUTODOCK 4.01 program was employed to perform automated molecular docking.

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Title: Evaluation of selective human MAO inhibitory activities of some novel pyrazoline derivatives
Authors: Umut Salgın-Gökşen
Samiye Yabanoğlu-Çiftçi
Ayşe Ercan
Kemal Yelekçi
Gülberk Uçar
Nesrin Gökhan-Kelekçi
Publication date: 01-06-2013
Publisher: Springer Vienna
Published in: Journal of Neural Transmission / Issue 6/2013
Print ISSN: 0300-9564
Electronic ISSN: 1435-1463
DOI: https://doi.org/10.1007/s00702-013-0980-6

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Evaluation of selective human MAO inhibitory activities of some novel pyrazoline derivatives

Abstract

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

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