Design, synthesis, molecular modelling and in vitro screening of monoamine oxidase inhibitory activities of novel quinazolyl hydrazine derivatives-Reference-Cited by-同舟云学术

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

Published:2020-04 Issue:4 Volume:7 Page:200050
ISSN:2054-5703
Container-title:Royal Society Open Science
language:en
Short-container-title:R. Soc. open sci.

Author:

Amer Adel¹²^ORCID,Hegazi Abdelrahman H.²^ORCID,Alshekh Mohammed Khalil¹,Ahmed Hany E. A.³⁴,Soliman Saied M.²^ORCID,Maniquet Antonin⁵,Ramsay Rona R.⁵^ORCID

Affiliation:

1. Department of Chemistry, College of Science, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia

2. Department of Chemistry, Faculty of Science, Alexandria University, Alexandria 21321, Egypt

3. Pharmacognosy and Pharmaceutical Chemistry Department, Pharmacy College, Taibah University, Al-Madinha Al-Munawarah, Saudi Arabia

4. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt

5. Biomedical Sciences Research Complex, University of St Andrews, Biomolecular Sciences Building, North Haugh, St Andrews KY16 9ST, UK

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 (4-hydroxy-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.

Funder

Deanship of Scientific Research at Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia

Publisher

The Royal Society

Subject

Multidisciplinary

Link

https://royalsocietypublishing.org/doi/pdf/10.1098/rsos.200050

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