In VitroandIn SilicoStudies of Quinoline-2-Carbaldehyde Hydrazone Derivatives as Potent Antimicrobial Agents

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dc.authoridUzunhisarcıklı, Ebru/0000-0002-7088-7490
dc.authoridcelik, ismail/0000-0002-8146-1663
dc.authoridCelik, Ismail/0000-0002-8146-1663;
dc.authorwosidUzunhisarcıklı, Ebru/AAS-9941-2021
dc.authorwosidİNCE, UFUK/AAT-3533-2021
dc.authorwosidINCE, Ufuk/KFT-0343-2024
dc.authorwosidPuskullu, Mustafa Orhan/AAO-1266-2021
dc.authorwosidcelik, ismail/AAX-3221-2020
dc.authorwosidCelik, Ismail/ABE-5813-2021
dc.authorwosidUzunhisarcıklı, Ebru/ADH-3056-2022
dc.contributor.authorCelik, Ismail
dc.contributor.authorErol, Meryem
dc.contributor.authorPuskullu, Mustafa Orhan
dc.contributor.authorUzunhisarcikli, Ebru
dc.contributor.authorInce, Ufuk
dc.contributor.authorKuyucuklu, Gulcan
dc.contributor.authorSuzen, Sibel
dc.date.accessioned2024-06-12T10:52:00Z
dc.date.available2024-06-12T10:52:00Z
dc.date.issued2022
dc.departmentTrakya Üniversitesien_US
dc.description.abstractWe previously synthesized a series of quinoline-2-carbaldehyde hydrazone derivatives and evaluated their antioxidant activities. In this study, the antimicrobial activities of these quinoline-2-carbaldehyde hydrazone derivatives were evaluated antimicrobial activity by the microdilution method, and there cytotoxic effect was investigated in MCF-7 and A549 cells by MTT assay. When the activity results were examined, although the antimicrobial activity of quinoline derivatives were equal or better than standard drugs in general, compound4(2 mu g/mL) and8(1 mu g/mL) againstE. faecalisand5(8 mu g/mL) againstP. aeruginosaare the most effective derivatives of the series. Besides, disk diffusion test was applied to these three compounds, and significant zone formation was observed at8(7 mm) compared to vancomycin (9 mm). Compounds showed no antiproliferative in A549 and MCF-7 cell lines, and compound4, 5,and8, which showed the most effective antimicrobial activity, were examined in healthy cells (Beas-2b) and no effect on cell viability was found. To understand the mechanism of this action of these compounds againstE. faecalis, molecular docking studies were performed on 15 different proteins, and it was concluded that the compounds interacted with FabH and not enough with other protein structures. The theoretical ADME profiles of compounds comply with Lipinski and other limiting rules. Also, some theoretical quantum parameters (HOMO-LUMO) of compounds, and both MEP analysis and geometric optimization analysis of8were calculated with 6-311 G (d,p) base set and DFT/B3LYP theory, and the results were shown.en_US
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK) Research and Development Grant [112S599]; Erciyes University Technology and Research Center (TAUM); TUBITAK [108S202]en_US
dc.description.sponsorshipThe chemical compounds of this work were supported by The Scientific and Technological Research Council of Turkey (TUBITAK) Research and Development Grant 112S599 and Erciyes University Technology and Research Center (TAUM). The cell culture facility was established by the support of TUBITAK 108S202 Grant.en_US
dc.identifier.doi10.1080/10406638.2020.1821230
dc.identifier.endpage1958en_US
dc.identifier.issn1040-6638
dc.identifier.issn1563-5333
dc.identifier.issue4en_US
dc.identifier.scopus2-s2.0-85091077459en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage1942en_US
dc.identifier.urihttps://doi.org/10.1080/10406638.2020.1821230
dc.identifier.urihttps://hdl.handle.net/20.500.14551/18566
dc.identifier.volume42en_US
dc.identifier.wosWOS:000569993200001en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Ltden_US
dc.relation.ispartofPolycyclic Aromatic Compoundsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAntimicrobial Activityen_US
dc.subjectEen_US
dc.subjectFaecalisen_US
dc.subjectMolecular Dockingen_US
dc.subjectQuinolineen_US
dc.subjectQuinoline Derivativesen_US
dc.subjectAntioxidanten_US
dc.subjectHardnessen_US
dc.titleIn VitroandIn SilicoStudies of Quinoline-2-Carbaldehyde Hydrazone Derivatives as Potent Antimicrobial Agentsen_US
dc.typeArticleen_US

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