da Silva_2016_J.Enzyme.Inhib.Med.Chem__1

Acetylcholinesterase inhibitors and compounds that trigger Abeta amyloid oligomerization and fibrillization represent an opportunity to discover new drug candidates to treat Alzheimer's disease. In this work, we synthesized nine new acylhydrazones and a known one, both employing 3-carboethoxy-4-quinolone derivatives as starting materials with chemical yields ranging from 63% to 90%. We evaluated the effect of these compounds on the acetylcholinesterase (AChE) activity and the fibrillization of Abeta42 peptide. Except for one acylhydrazone, the compounds exhibited good inhibitory effect on AChE (1.2 muM < IC50 values < 17 muM). They also showed a significant decrease in the thioflavin-T fluorescence emission, suggesting an inhibitory effect on the Abeta42 fibril formation.