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Type: Artigo
Title: Effects Of Novel Acylhydrazones Derived From 4-quinolone On The Acetylcholinesterase Activity And A Beta 42 Peptide Fibrils Formation
Author: da Silva
Gisele S.; Figueiro
Micheli; Tormena
Claudio F.; Coelho
Fernando; Almeida
Wanda P.
Abstract: Acetylcholinesterase inhibitors and compounds that trigger Ab 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 A beta(42) peptide. Except for one acylhydrazone, the compounds exhibited good inhibitory effect on AChE (1.2 mu M < IC50 values < 17 mu M). They also showed a significant decrease in the thioflavin-T fluorescence emission, suggesting an inhibitory effect on the A beta(42) fibril formation.
Subject: Acetylcholinesterase
Alzheimer's Disease
Editor: Taylor & Francis Ltd
Citation: Journal Of Enzyme Inhibition And Medicinal Chemistry. Taylor & Francis Ltd, v. 31, p. 1464 - 1470, 2016.
Rights: fechado
Identifier DOI: 10.3109/14756366.2016.1144597
Date Issue: 2016
Appears in Collections:Unicamp - Artigos e Outros Documentos

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