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

Autor: Adel Amer, Abdelrahman H. Hegazi, Mohammed Khalil Alshekh, Hany E. A. Ahmed, Saied M. Soliman, Antonin Maniquet, Rona R. Ramsay
Jazyk: angličtina
Rok vydání: 2020
Předmět:
Zdroj: Royal Society Open Science, Vol 7, Iss 4 (2020)
Druh dokumentu: article
ISSN: 2054-5703
DOI: 10.1098/rsos.200050
Popis: 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.
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