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Synthesis of new quinoline-piperonal hybrids as potential drugs against Alzheimer’s disease

International Journal of Molecular Sciences, ISSN: 1422-0067, Vol: 20, Issue: 16
2019
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Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Disease.

Int J Mol Sci. 2019 Aug 14;20(16) Authors: de Oliveira C Brum J, Neto DC, de Almeida JS, Lima JA, Kuca K, França TC, Figueroa-Villar JD PubMed: 31416113 Submit Comment

Article Description

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.

Bibliographic Details

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

MDPI AG

Chemical Engineering; Biochemistry, Genetics and Molecular Biology; Chemistry; Computer Science

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