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

Brum, Juliana de Oliveira C.; Neto, Denise Cristian F.; de Almeida, Joyce Sobreiro E. D.; Lima, Joselia Alencar; Kuča, Kamil; Costa Franca, Tanos Celmar; Figueroa-Villar, Jose D.

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dc.rights.license	CC BY	eng
dc.contributor.author	Brum, Juliana de Oliveira C.	cze
dc.contributor.author	Neto, Denise Cristian F.	cze
dc.contributor.author	de Almeida, Joyce Sobreiro E. D.	cze
dc.contributor.author	Lima, Joselia Alencar	cze
dc.contributor.author	Kuča, Kamil	cze
dc.contributor.author	Costa Franca, Tanos Celmar	cze
dc.contributor.author	Figueroa-Villar, Jose D.	cze
dc.date.accessioned	2020-06-05T12:52:04Z
dc.date.available	2020-06-05T12:52:04Z
dc.date.issued	2019	eng
dc.identifier.issn	1661-6596	eng
dc.identifier.uri	http://hdl.handle.net/20.500.12603/318
dc.description.abstract	Six 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.format	p. "Article Number: 3944"	eng
dc.language.iso	eng	eng
dc.publisher	MDPI-Molecular diversity preservation international	eng
dc.relation.ispartof	International journal of molecular sciences, volume 20, issue: 16	eng
dc.subject	piperonal	eng
dc.subject	quinolines	eng
dc.subject	guanil-hydrazones	eng
dc.subject	acetylcholinesterase	eng
dc.subject	Alzheimer's disease	eng
dc.subject	piperonal	cze
dc.subject	chinoliny	cze
dc.subject	guanil-hydrazony	cze
dc.subject	acetylcholinesteráza	cze
dc.subject	Alzheimerova choroba	cze
dc.title	Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Disease	eng
dc.title.alternative	Syntéza nových chinolin-piperidálních hybridů jako potenciálních léčiv proti Alzheimerově chorobě	cze
dc.type	article	eng
dc.identifier.obd	43875531	eng
dc.identifier.wos	000484411100101	eng
dc.identifier.doi	10.3390/ijms20163944	eng
dc.description.abstract-translated	Six 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.publicationstatus	postprint	eng
dc.peerreviewed	yes	eng
dc.source.url	https://www.mdpi.com/1422-0067/20/16/3944/htm	cze
dc.relation.publisherversion	https://www.mdpi.com/1422-0067/20/16/3944/htm	eng
dc.rights.access	Open Access	eng