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- Title
Synthesis of New Quinoline-Piperonal Hybrids as Potential Drugs against Alzheimer's Disease.
- 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.
- 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.
- Subjects
ALZHEIMER'S disease; BLOOD-brain barrier
- Publication
International Journal of Molecular Sciences, 2019, Vol 20, Issue 16, p3944
- ISSN
1661-6596
- Publication type
Article
- DOI
10.3390/ijms20163944