Current Bioactive Compounds

Adriano Mollica
Department of Pharmacy, University ”G. d' Annunzio” of Chieti-Pescara
Via dei Vestini 31
Chieti, 66100
Italy

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

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

Abstract:

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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Article Details

VOLUME: 4
ISSUE: 3
Year: 2008
Page: [159 - 174]
Pages: 16
DOI: 10.2174/157340708786305970
Price: $58