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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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dc.contributor.authorAmer, Adel
dc.contributor.authorHegazi, Abdelrahman H.
dc.contributor.authorAlshekh, Mohammed Khalil
dc.contributor.authorAhmed, Hany Emary Ali
dc.contributor.authorSoliman, Saied M.
dc.contributor.authorManiquet, Antonin
dc.contributor.authorRamsay, Rona R.
dc.date.accessioned2020-05-11T15:30:04Z
dc.date.available2020-05-11T15:30:04Z
dc.date.issued2020-04-22
dc.identifier.citationAmer , 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.200050en
dc.identifier.issn2054-5703
dc.identifier.otherPURE: 266738560
dc.identifier.otherPURE UUID: e5842536-adfe-4524-93bf-e9f52611a8e9
dc.identifier.otherORCID: /0000-0003-1535-4904/work/74117685
dc.identifier.otherWOS: 000546929500015
dc.identifier.otherScopus: 85084820830
dc.identifier.urihttps://hdl.handle.net/10023/19917
dc.descriptionFunding: Deanship of Scientific Research at Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia (project # 7101).en
dc.description.abstractA 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.
dc.format.extent18
dc.language.isoeng
dc.relation.ispartofRoyal Society Open Scienceen
dc.rightsCopyright © 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.en
dc.subjectStructure-activity relationshipsen
dc.subjectQuinazoline analoguesen
dc.subjectAntidepressanten
dc.subjectMonoamine oxidase inhibitorsen
dc.subjectQD Chemistryen
dc.subjectQH301 Biologyen
dc.subjectRC0321 Neuroscience. Biological psychiatry. Neuropsychiatryen
dc.subjectRM Therapeutics. Pharmacologyen
dc.subjectChemistry(all)en
dc.subjectDASen
dc.subject.lccQDen
dc.subject.lccQH301en
dc.subject.lccRC0321en
dc.subject.lccRMen
dc.titleDesign, synthesis, molecular modelling and in vitro screening of monoamine oxidase inhibitory activities of novel quinazolyl hydrazine derivativesen
dc.typeJournal articleen
dc.description.versionPublisher PDFen
dc.contributor.institutionUniversity of St Andrews. School of Biologyen
dc.contributor.institutionUniversity of St Andrews. Biomedical Sciences Research Complexen
dc.identifier.doihttps://doi.org/10.1098/rsos.200050
dc.description.statusPeer revieweden


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