Antimicrobial and antiproliferative activity studies of some new quinoline-3-carbaldehyde hydrazone derivatives

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dc.authoridCelik, Ismail/0000-0002-8146-1663
dc.authoridUzunhisarcıklı, Ebru/0000-0002-7088-7490
dc.authoridcelik, ismail/0000-0002-8146-1663
dc.authoridFatullayev, Hanifa/0000-0002-7123-8396
dc.authoridKUYUCUKLU, GÜLCAN/0000-0003-1596-1659
dc.authorwosidCelik, Ismail/ABE-5813-2021
dc.authorwosidUzunhisarcıklı, Ebru/AAS-9941-2021
dc.authorwosidUzunhisarcıklı, Ebru/ADH-3056-2022
dc.authorwosidFatullayev, Hanifa/JXM-8094-2024
dc.authorwosidPuskullu, Mustafa Orhan/AAO-1266-2021
dc.authorwosidcelik, ismail/AAX-3221-2020
dc.authorwosidFatullayev, Hanifa/R-8111-2018
dc.contributor.authorPuskullu, Mustafa Orhan
dc.contributor.authorCelik, Ismail
dc.contributor.authorErol, Meryem
dc.contributor.authorFatullayev, Hanifa
dc.contributor.authorUzunhisarcikli, Ebru
dc.contributor.authorKuyucuklu, Gulcan
dc.date.accessioned2024-06-12T11:13:21Z
dc.date.available2024-06-12T11:13:21Z
dc.date.issued2020
dc.departmentTrakya Üniversitesien_US
dc.description.abstractIn this study, a total of 22 piece quinoline-3-carbaldehyde hydrazone derivative compounds were designed and synthesized, 2 of which were not original, their antimicrobial activities were determined with microdilution method and their in vitro cytotoxic effect was investigated in MCF-7 and A549 cells by MTT assay. When the activity results are examined, although the antimicrobial effects of quinoline derivatives, in general, are weaker than standard drugs; 3q5 and 3q6 against MRSA showed promising activity with MIC:16 mu g/ml compared to reference drugs. Compounds generally showed weaker cytotoxic activity on the A549 and MCF-7 cell line. 3q12, 3q17 and 3q22 at 100 mu M reduced cell viability to 59.28%, 76.24% and 72.92% on A549 cells, respectively. Compound 3q6, one of the most effective compounds against MRSA, formed a 2.10 angstrom long hydrogen bond between the quinoline nitrogen and ARG132 in the DNA topoisomerase IV active site (PDB: 3FV5). Theoretical ADME profiles of all compounds comply with Lipinski and other limiting rules. In addition, MEP analysis of 3q6, geometric optimization and molecular reactivity analysis were calculated with the 6-311G (d,p) base set DFT/ B3LYP theory, and Delta E = ELUMO-EHOMO, which is a measure of the stable structure of the molecule, was cal-culated as 0.13377 for 3q6 and had the most stable electronic structure among all compounds.en_US
dc.description.sponsorshipErciyes University Scientific Research Projects Coordination Unit [TSA-2019-9442, THD-2019-8849]en_US
dc.description.sponsorshipThis work has been supported by Erciyes University Scientific Research Projects Coordination Unit with research projects TSA-2019-9442 and THD-2019-8849. NMR analysis of the compounds was performed by Erciyes University Technology and Research Center (TAUM) and HRMS analysis was performed by Bilkent University National Nanotechnology Research Center (UNAM).en_US
dc.identifier.doi10.1016/j.bioorg.2020.104014
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid32599364en_US
dc.identifier.scopus2-s2.0-85086850874en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2020.104014
dc.identifier.urihttps://hdl.handle.net/20.500.14551/23503
dc.identifier.volume101en_US
dc.identifier.wosWOS:000552635800009en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherAcademic Press Inc Elsevier Scienceen_US
dc.relation.ispartofBioorganic Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectQuinolineen_US
dc.subjectHydrazoneen_US
dc.subjectAntimicrobial Activityen_US
dc.subjectCytotoxicityen_US
dc.subjectMolecular Dockingen_US
dc.subjectSpectroscopic Investigationsen_US
dc.subjectThermal-Propertiesen_US
dc.subjectComplexesen_US
dc.subjectBindingen_US
dc.titleAntimicrobial and antiproliferative activity studies of some new quinoline-3-carbaldehyde hydrazone derivativesen_US
dc.typeArticleen_US

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