Design, synthesis, structure, toxicology and in vitro testing of three novel agents for Alzheimer’s disease

Figueroa‐Villar, José Daniel

doi:10.1039/c6ra27042e

Cited by 3 publications

(1 citation statement)

References 25 publications

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“…Recent published works have indicated results consistent with Ellman’s method [25,32,33,34,35,36]. In our study we used the NMR method [29] to determine the concentrations of the substrate (ACh) and the product acetate (Ac), which are obtained from direct integration of the corresponding absorption peaks for methyl groups (2.24 ppm for ACh and 2.16 ppm for Ac) [32,35]. The comparison between the integration of the Ac peak in pure AChE (no inhibitor) and in the presence of the inhibitor allowed the determination of the percentages of inhibition shown in the plot of Figure 3.…”

Section: Resultsmentioning

confidence: 69%

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

Brum

Neto

Almeida

et al. 2019

IJMS

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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.

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