N-Substituted piperidine-3-carbohydrazide-hydrazones against Alzheimer's disease: Synthesis and evaluation of cholinesterase, beta-amyloid inhibitory activity, and antioxidant capacity

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dc.authoridTarikogullari, Ayse H/0000-0002-3134-2754
dc.authoridparlar, sulunay/0000-0002-2892-5932
dc.authoridAlan Albayrak, Elif/0000-0001-9636-4068
dc.authorscopusid35293209900
dc.authorscopusid57204901858
dc.authorscopusid6505793953
dc.authorscopusid56685676600
dc.authorscopusid57329388100
dc.authorscopusid8970943500
dc.authorscopusid6603583717
dc.authorwosidTarikogullari, Ayse H/IWD-5182-2023
dc.authorwosidparlar, sulunay/HLH-0355-2023
dc.contributor.authorParlar, Sulunay
dc.contributor.authorSayar, Gözde
dc.contributor.authorTarıkoğulları, Ayse H. H.
dc.contributor.authorSözer Karadağlı, Sumru
dc.contributor.authorAlan, Elif
dc.contributor.authorSevin, Gülnur
dc.contributor.authorErciyas, Ercin
dc.date.accessioned2024-08-25T18:36:12Z
dc.date.available2024-08-25T18:36:12Z
dc.date.issued2023
dc.departmentEge Üniversitesien_US
dc.description.abstractA series of piperidine-3-carbohydrazide-hydrazones bearing phenylethyl, phenylpropyl, and phenylbutyl substituents on piperidine nitrogen were designed and synthesized as cholinesterase (ChE) inhibitors. The title compounds were screened for acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) inhibitory activities and antioxidant capacities, and the active ones for A beta(42) self-aggregation inhibition, in vitro. The chemiluminescence method was used to determine the effect of the selected compounds on the reactive oxygen species (ROS) levels in brain tissue. Physicochemical properties were calculated by the MOE program. Kinetic analysis and molecular modeling studies were also carried out for the most active compounds. Generally, the final compounds exhibited moderate to good AChE or BuChE inhibitory activity. Among them, 3g and 3j showed the most potent activity against AChE (IC50 = 4.32 mu M) and BuChE (IC50 = 1.27 mu M), respectively. The kinetic results showed that both compounds exhibited mixed-type inhibition. Among the selected compounds, nitro derivatives (3g, 4g, and 5g) provided better A beta(42) inhibition. According to the chemiluminescence assay, 4i exhibited the most active superoxide free-radical scavenger activity and 3g, 3j, and 4i showed similar scavenger activity on other ROS. All results suggested that 3g, 3j, and 4i have good AChE/BuChE, A beta(42) inhibitory potentials and antioxidant capacities and can therefore be suggested as promising multifunctional agents to combat Alzheimer's disease.en_US
dc.description.sponsorshipTUBITAK (The Scientific and Technological Research Council of Turkey) [214S083]; Pharmaceutical Sciences Research Centre (FABAL) at Ege Universityen_US
dc.description.sponsorshipThis project was supported by TUBITAK (The Scientific and Technological Research Council of Turkey), Project Number: 214S083. The authors would like to thank the Pharmaceutical Sciences Research Centre (FABAL) at Ege University Faculty of Pharmacy for spectral and elemental analyses of the compounds.en_US
dc.identifier.doi10.1002/ardp.202200519
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue3en_US
dc.identifier.pmid36461719en_US
dc.identifier.scopus2-s2.0-85143536175en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/ardp.202200519
dc.identifier.urihttps://hdl.handle.net/11454/100557
dc.identifier.volume356en_US
dc.identifier.wosWOS:000970251200009en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofArchiv Der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmz20240825_Gen_US
dc.subjectacetylcholinesterase inhibitoryen_US
dc.subjectantioxidant activityen_US
dc.subjectbutyrylcholinesterase inhibitoryen_US
dc.subjectkinetic studyen_US
dc.subjectmolecular modelingen_US
dc.subjectthioflavin T testen_US
dc.subjectTarget-Directed Ligandsen_US
dc.subjectAcetylcholinesterase Inhibitorsen_US
dc.subjectHybridsen_US
dc.subjectDesignen_US
dc.subjectAlgorithmen_US
dc.subjectPeptidesen_US
dc.subjectWateren_US
dc.titleN-Substituted piperidine-3-carbohydrazide-hydrazones against Alzheimer's disease: Synthesis and evaluation of cholinesterase, beta-amyloid inhibitory activity, and antioxidant capacityen_US
dc.typeArticleen_US

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