New amyloid beta-disaggregating agents: synthesis, pharmacological evaluation, crystal structure and molecular docking of N-(4-((7-chloroquinolin-4-yl)oxy)-3-ethoxybenzyl)amines.

ABSTRACT: In the journey towards the development of potent multi-targeted ligands for the treatment of Alzheimer's disease, a series of Aβ aggregation inhibitors having quinoline scaffold were designed utilizing computational biology tools, synthesized and characterized by various spectral techniques including single-crystal X-ray crystallography. Organic syntheses relying upon convergent synthetic routes were employed. Investigations via ThT fluorescence assay, electron microscopy and transmission electron microscopy revealed the synthesized derivatives to exhibit Aβ self-aggregation inhibition. Molecules 5g and 5a showed the highest inhibitory potential, 53.73% and 53.63% at 50 μM respectively; higher than the standard Aβ disaggregating agent, curcumin. Molecules 5g and

SUBMITTER: Umar T 

PROVIDER: S-EPMC6254049 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature