Synthesis and Screening of Human Monoamine Oxidase-A Inhibitor Effect of New 2-Pyrazoline and Hydrazone Derivatives

dc.contributor.authorYelekçi, Kemal
dc.contributor.authorBaysal, İpek
dc.contributor.authorYabanoğlu-Çiftçi, Samiye
dc.contributor.authorDjikic, Teodora
dc.contributor.authorYelekçi, Kemal
dc.contributor.authorUçar, Gülberk
dc.contributor.authorErtan, Rahmiye
dc.date.accessioned2019-06-27T08:02:11Z
dc.date.available2019-06-27T08:02:11Z
dc.date.issued2015
dc.departmentFakülteler, Mühendislik ve Doğa Bilimleri Fakültesi, Biyoinformatik ve Genetik Bölümüen_US
dc.description.abstractA group of 35-diaryl-2-pyrazoline and hydrazone derivatives was prepared via the reaction of various chalcones with hydrazide compounds in ethanol. Twenty original compounds were synthesized. Ten of these original compounds have a pyrazoline structure nine of these original compounds have a hydrazone structure and one of these original compounds has a chalcone structure. Structural elucidation of the compounds was performed by IR H-1 NMR C-13 NMR mass spectral data and elemental analyses. These compounds were tested for their inhibitory activities toward the A and B isoforms of human monoamine oxidase (MAO). Except for 3k and 6c all compounds were found to be competitive reversible and selective inhibitors for either one of the isoforms (hMAO-A or MAO-B). Compounds 3k and 6c were found to be competitive reversible but non-selective MAO inhibitors. Compound 6h showed hMAO-B inhibitory activity whereas the others potently inhibited hMAO-A. Compound 5c showed higher selectivity than the standard drug moclobemide. According to the experimental K-i values compounds 6i 6d and 6a exhibited the highest inhibitory activity toward hMAO-A. The AutoDock 4.2 program was employed to perform automated molecular docking. The calculated results obtained computationally were in good agreement with the experimental values.en_US]
dc.identifier.citation20
dc.identifier.doi10.1002/ardp.201500212en_US
dc.identifier.endpage756
dc.identifier.issn0365-6233en_US
dc.identifier.issn1521-4184en_US
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue10
dc.identifier.pmid26293971en_US
dc.identifier.scopus2-s2.0-84942987491en_US
dc.identifier.scopusqualityQ2
dc.identifier.startpage743en_US
dc.identifier.urihttps://hdl.handle.net/20.500.12469/569
dc.identifier.urihttps://doi.org/10.1002/ardp.201500212
dc.identifier.volume348en_US
dc.identifier.wosWOS:000362565600006en_US
dc.identifier.wosqualityN/A
dc.institutionauthorYelekçi, Kemalen_US
dc.language.isoenen_US
dc.publisherWiley-VCH Verlag GmbHen_US
dc.relation.journalArchiv Der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subject2-Pyrazolineen_US
dc.subjectHydrazoneen_US
dc.subjectMAO inhibitorsen_US
dc.subjectMolecular dockingen_US
dc.titleSynthesis and Screening of Human Monoamine Oxidase-A Inhibitor Effect of New 2-Pyrazoline and Hydrazone Derivativesen_US
dc.typeArticleen_US
dspace.entity.typePublication
relation.isAuthorOfPublication9407938e-3d31-453b-9199-aaa8280a66c5
relation.isAuthorOfPublication.latestForDiscovery9407938e-3d31-453b-9199-aaa8280a66c5

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