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Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Disease

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dc.contributor.authorBrum, Juliana de Oliveira C.
dc.contributor.authorNeto, Denise Cristian F.
dc.contributor.authorde Almeida, Joyce Sobreiro E. D.
dc.contributor.authorLima, Joselia Alencar
dc.contributor.authorKuča, Kamil
dc.contributor.authorCosta Franca, Tanos Celmar
dc.contributor.authorFigueroa-Villar, Jose D.
dc.date.accessioned2020-06-05T12:52:04Z
dc.date.available2020-06-05T12:52:04Z
dc.date.issued2019
dc.description.abstractSix quinoline-piperonal hybrids were synthesized and evaluated as potential drugs against Alzheimer's disease (AD). Theoretical analysis of the pharmacokinetic and toxicological properties of the compounds suggest that they present good oral bio-availability and are also capable of penetrating the blood-brain barrier, qualifying as leads for new drugs against AD. Evaluation of their inhibitory capacity against acetyl- and butyrilcholinesterases (AChE and BChE) through Ellmann's test showed that three compounds present promising results with one of them being capable of inhibiting both enzymes. Further docking studies of the six compounds synthesized helped to elucidate the main interactions that may be responsible for the inhibitory activities observed.eng
dc.description.abstract-translatedSix quinoline-piperonal hybrids were synthesized and evaluated as potential drugs against Alzheimer's disease (AD). Theoretical analysis of the pharmacokinetic and toxicological properties of the compounds suggest that they present good oral bio-availability and are also capable of penetrating the blood-brain barrier, qualifying as leads for new drugs against AD. Evaluation of their inhibitory capacity against acetyl- and butyrilcholinesterases (AChE and BChE) through Ellmann's test showed that three compounds present promising results with one of them being capable of inhibiting both enzymes. Further docking studies of the six compounds synthesized helped to elucidate the main interactions that may be responsible for the inhibitory activities observed.cze
dc.formatp. &quot;Article Number: 3944&quot;
dc.identifier.doi10.3390/ijms20163944
dc.identifier.issn1661-6596
dc.identifier.obd43875531
dc.identifier.urihttp://hdl.handle.net/20.500.12603/318
dc.identifier.wos000484411100101
dc.language.isoeng
dc.peerreviewedyes
dc.publicationstatuspostprint
dc.publisherMDPI-Molecular diversity preservation international
dc.relation.ispartofInternational journal of molecular sciences, volume 20, issue: 16eng
dc.relation.publisherversionhttps://www.mdpi.com/1422-0067/20/16/3944/htm
dc.rights.accessOpen Access
dc.rights.licenseCC BY
dc.source.urlhttps://www.mdpi.com/1422-0067/20/16/3944/htm
dc.subjectpiperonaleng
dc.subjectquinolineseng
dc.subjectguanil-hydrazoneseng
dc.subjectacetylcholinesteraseeng
dc.subjectAlzheimer's diseaseeng
dc.subjectpiperonalcze
dc.subjectchinolinycze
dc.subjectguanil-hydrazonycze
dc.subjectacetylcholinesterázacze
dc.subjectAlzheimerova chorobacze
dc.titleSynthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Diseaseeng
dc.title.alternativeSyntéza nových chinolin-piperidálních hybridů jako potenciálních léčiv proti Alzheimerově choroběcze
dc.typearticle

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