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Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer’s Disease
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Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer’s Disease
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Journal Article
Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer’s Disease
2019
Overview
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.
Publisher
MDPI AG,MDPI
Subject
/ Alzheimer Disease - drug therapy
/ Alzheimer Disease - metabolism
/ Chemistry Techniques, Synthetic
/ Cholinesterase Inhibitors - chemical synthesis
/ Cholinesterase Inhibitors - chemistry
/ Cholinesterase Inhibitors - pharmacokinetics
/ Cholinesterase Inhibitors - pharmacology
/ Drugs
/ Enzymes
/ Humans
/ Kinetics
/ Magnetic Resonance Spectroscopy
/ Molecular Docking Simulation
/ Molecular Dynamics Simulation
/ Solvents
