Design, synthesis, molecular modelling and in vitro screening of monoamine oxidase inhibitory activities of novel quinazolyl hydrazine derivatives

Adel Amer; Abdelrahman H. Hegazi; Mohammed Khalil Alshekh; Hany E. A. Ahmed; Saied M. Soliman; Antonin Maniquet; Rona R. Ramsay

doi:10.1098/rsos.200050

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Design, synthesis, molecular modelling and in vitro screening of monoamine oxidase inhibitory activities of novel quinazolyl hydrazine derivatives

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Design, synthesis, molecular modelling and in vitro screening of monoamine oxidase inhibitory activities of novel quinazolyl hydrazine derivatives

Adel Amer, Abdelrahman H. Hegazi, Mohammed Khalil Alshekh, Hany E. A. Ahmed, Saied M. Soliman, Antonin Maniquet and Rona R. Ramsay

Royal Society open science, Vol.7(4), pp.200050-200050

01/04/2020

DOI: https://doi.org/10.1098/rsos.200050

PMID: 32431898

Abstract

Multidisciplinary Sciences

Science & Technology

Science & Technology - Other Topics

A new series of N'-substituted benzylidene-2-(4-oxo-2-phenyl-1,4-dihydroquinazolin-3(2H)-ypacetohydrazide (5a-5h) has been synthesized, characterized by FT-IR, NMR spectroscopy and mass spectrometry and tested against human monoamine oxidase (MAO) A and B. Only (4-hyclroxy-3-methoxybenzylidene) substituted compounds gave submicromolar inhibition of MAO-A and MAO-B. Changing the phenyl substituent to methyl on the unsaturated quinazoline ring (12a-12d) decreased inhibition, but a less flexible linker (14a-14d) resulted in selective micromolar inhibition of hMAO-B providing insight for ongoing design. [GRAPHICS] .

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Title: Design, synthesis, molecular modelling and in vitro screening of monoamine oxidase inhibitory activities of novel quinazolyl hydrazine derivatives
Creators - without role: Adel Amer - Taibah University
Abdelrahman H. Hegazi - Alexandria University
Mohammed Khalil Alshekh - Taibah University
Hany E. A. Ahmed - Taibah University
Saied M. Soliman - Alexandria University
Antonin Maniquet - University of St Andrews
Rona R. Ramsay - University of St Andrews
Publication Details: Royal Society open science, Vol.7(4), pp.200050-200050
Publisher: Royal Soc London
Number of pages: 18
Grant note: 7101 / Deanship of Scientific Research at Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia
Identifiers: 9929707608331
Academic Unit: Taibah University
Language: English
Resource Type: Journal article