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dc.contributor.authorKaraman, Nurcan
dc.contributor.authorSıcak, Yusuf
dc.contributor.authorTaşkın-Tok, Tuğba
dc.contributor.authorÖztürk, Mehmet
dc.contributor.authorKarakuçuk-İyidoğan, Ayşegül
dc.contributor.authorDikmen, Miriş
dc.contributor.authorOruç-Emre, Emine Elçin
dc.date.accessioned2019-10-19T14:16:36Z
dc.date.available2019-10-19T14:16:36Z
dc.date.issued2016
dc.identifier.issn0223-5234
dc.identifier.issn1768-3254
dc.identifier.urihttps://dx.doi.org/10.1016/j.ejmech.2016.08.037
dc.identifier.urihttps://hdl.handle.net/11421/13193
dc.descriptionWOS: 000388544600022en_US
dc.descriptionPubMed ID: 27592396en_US
dc.description.abstractHydrazones and the piperidine ring containing compounds were considered as beneficial substrates in drug design. Therefore, this study was aimed at the synthesis of new benzoyl hydrazones derived from ethyl 4-oxopiperidine-1-carboxylate and 2,6-diphenylpiperidin-4-one. The synthesized compounds (1-19) were screened for their antioxidant, anticholinesterase and anticancer activities. The antioxidant capacity of the compounds was evaluated by using four complementary tests. The results showed that compound 7 and 17 have the higher lipid peroxidation inhibitory activity than the other compounds. In DPPH scavenging assay, compounds 5, 6, 10,14, 17 demonstrated better activity than that of standard BHT, while in ABTS(+) scavenging assay compound 6 and 17 exhibited better activity among the other compounds. The CUPRAC assay disclosed that compound 2 displayed better activity than alpha-tocopherol. The anticholinesterase activity was performed against acetylcholinesterase (AChE) and butyrylcholinesterase.(BChE) enzymes. Compound 11 (IC50: 35.30 +/- 1.11 mu M) inhibited BChE better than galantamine (IC50: 46.03 0.14 mu M). We conclude that the compound 11 can be considered as a candidate for BChE inhibitor. Moreover docking method was applied to elucidate the AChE and BChE inhibitory mechanism of the compound 11. Molecular docking analysis revealed that compound 11 bound to BChE enzyme more efficiently when compared to the AChE due to its orientations and different types of interactions. In addition, the non-cytotoxic properties of the compounds brought them into prominence, although they did not show significant anticancer propertiesen_US
dc.description.sponsorshipGaziantep University Scientific Research Projects Governing Unit (BAPYB), Turkiye [FEF.11.03]en_US
dc.description.sponsorshipThis study was supported by the Gaziantep University Scientific Research Projects Governing Unit (BAPYB) (Project no: FEF.11.03), Turkiye.en_US
dc.language.isoengen_US
dc.publisherElsevier France-Editions Scientifiques Medicales Elsevieren_US
dc.relation.isversionof10.1016/j.ejmech.2016.08.037en_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectPiperidineen_US
dc.subjectHydrazoneen_US
dc.subjectAnticholinesterase Activityen_US
dc.subjectAntioxidant Activityen_US
dc.subjectMolecular Dockingen_US
dc.titleNew piperidine-hydrazone derivatives: Synthesis, biological evaluations and molecular docking studies as AChE and BChE inhibitorsen_US
dc.typearticleen_US
dc.relation.journalEuropean Journal of Medicinal Chemistryen_US
dc.contributor.departmentAnadolu Üniversitesi, Eczacılık Fakültesi, Farmakoloji Anabilim Dalıen_US
dc.identifier.volume124en_US
dc.identifier.startpage270en_US
dc.identifier.endpage283en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.contributor.institutionauthorDikmen, Miriş


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