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Current Bioactive Compounds


ISSN (Print): 1573-4072
ISSN (Online): 1875-6646

Chemistry of Small Molecule Inhibitors in Self-Assembly of Alzheimers Disease Related Amyloid-Beta Peptide

Author(s): Bela Torok, Sujaya Dasgupta and Marianna Torok

Volume 4, Issue 3, 2008

Page: [159 - 174] Pages: 16

DOI: 10.2174/157340708786305970

Price: $65


The role of the chemical structure, namely the effect of substituents, of small molecule inhibitors in selfassembly of Alzheimers disease related amyloid-beta peptide is discussed. The literature analysis is concentrated on the past 10 years and analyzed the structure of Aβ inhibitors pointing out common features. A basis set of 321 compounds is reviewed and a chemical map of the inhibitors is provided highlighting the most common substituents that appear in these molecules. Based on the findings, aromatic/heteroaromatic groups were found to be present in an overwhelming majority of inhibitors (95%). Acidic substituents appeared the second most common substituent group (67%) suggesting the importance of these motifs as possible binding units. Several structure activity relationship studies that support this role are also discussed.

Keywords: Alzheimer's disease, amyloid, amyloid-beta peptide, self-assembly, fibrillogenesis, small molecule inhibitors, structure-activity relationship

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