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

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...

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Bibliographic Details
Published in:	International journal of molecular sciences Vol. 20; no. 16; p. 3944
Main Authors:	de Oliveira C Brum, Juliana, Neto, Denise Cristian F, de Almeida, Joyce Sobreiro F D, Lima, Josélia Alencar, Kuca, Kamil, França, Tanos Celmar C, Figueroa-Villar, José D
Format:	Journal Article
Language:	English
Published:	Switzerland MDPI AG 14-08-2019 MDPI
Subjects:	Acetone acetylcholinesterase Acids Aldehydes Alzheimer Disease - drug therapy Alzheimer Disease - metabolism Alzheimer's disease Benzaldehydes - chemistry Benzodioxoles - chemistry Bioavailability Carbonyl compounds Carbonyl groups Carbonyls Catalysis Central nervous system Chemistry Techniques, Synthetic Cholinesterase Inhibitors - chemical synthesis Cholinesterase Inhibitors - chemistry Cholinesterase Inhibitors - pharmacokinetics Cholinesterase Inhibitors - pharmacology Condensates Drugs Enzymes guanil-hydrazones Humans Hybrids Kinetics Magnetic Resonance Spectroscopy Molecular Docking Simulation Molecular Dynamics Simulation Molecular Structure Pharmacokinetics Piperonal Protonation Quinoline quinolines Quinolines - chemistry Solvents Structure-Activity Relationship acetylcholinesterase Alzheimer’s disease guanil-hydrazones quinolines piperonal
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Summary:	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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	1422-0067 1661-6596 1422-0067
DOI:	10.3390/ijms20163944