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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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Amer_2020_Design_synthesis_molecular_RSOS_200050_CC.pdf (13.59Mb)
Date
22/04/2020
Author
Amer, Adel
Hegazi, Abdelrahman H.
Alshekh, Mohammed Khalil
Ahmed, Hany Emary Ali
Soliman, Saied M.
Maniquet, Antonin
Ramsay, Rona R.
Keywords
Structure-activity relationships
Quinazoline analogues
Antidepressant
Monoamine oxidase inhibitors
QD Chemistry
QH301 Biology
RC0321 Neuroscience. Biological psychiatry. Neuropsychiatry
RM Therapeutics. Pharmacology
Chemistry(all)
DAS
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Abstract
A new series of N'-substituted benzylidene-2-(4-oxo-2-phenyl-1,4-dihydroquinazolin-3(2H)-yl)acetohydrazide (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 (3-methoxy-4-hydroxy)benzoyl 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.
Citation
Amer , A , Hegazi , A H , Alshekh , M K , Ahmed , H E A , Soliman , S M , Maniquet , A & Ramsay , R R 2020 , ' Design, synthesis, molecular modelling and in vitro screening of monoamine oxidase inhibitory activities of novel quinazolyl hydrazine derivatives ' , Royal Society Open Science , vol. 7 , 200050 . https://doi.org/10.1098/rsos.200050
Publication
Royal Society Open Science
Status
Peer reviewed
DOI
https://doi.org/10.1098/rsos.200050
ISSN
2054-5703
Type
Journal article
Rights
Copyright © 2020 The Authors. Published by the Royal Society under the terms of the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/, which permits unrestricted use, provided the original author and source are credited.
Description
Funding: Deanship of Scientific Research at Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia (project # 7101).
Collections
  • University of St Andrews Research
URI
http://hdl.handle.net/10023/19917

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