Please use this identifier to cite or link to this item:
|Title:||Effects Of Novel Acylhydrazones Derived From 4-quinolone On The Acetylcholinesterase Activity And A Beta 42 Peptide Fibrils Formation|
Effects of novel acylhydrazones derived from 4-quinolone on the acetylcholinesterase activity and Aβ42 peptide fibrils formation
|Author:||Silva, Gisele S. da|
Tormena, Cláudio F.
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.|
Acetylcholinesterase inhibitors and compounds that trigger Aβ 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 know
Alzheimer, Doença de
|Editor:||Taylor & Francis|
|Citation:||Journal Of Enzyme Inhibition And Medicinal Chemistry. Taylor & Francis Ltd, v. 31, p. 1464 - 1470, 2016.|
|Appears in Collections:||IQ - Artigos e Outros Documentos|
FCF - Artigos e Outros Documentos
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.