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Synthesis and Evaluation of New Cyclodextrin Derivatives as Amyloid‐β Aggregation Inhibitors
Author(s) -
Oliveri Valentina,
Vecchio Graziella
Publication year - 2019
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201902402
Subject(s) - moiety , chemistry , cyclodextrin , conjugated system , amyloid (mycology) , extracellular , combinatorial chemistry , biophysics , stereochemistry , biochemistry , organic chemistry , polymer , biology , inorganic chemistry
The presence of extracellular amyloid‐beta (Aβ) plaques is one of the pathological hallmarks of Alzheimer's disease. Appropriately functionalized compounds can modulate amyloidogenesis. Here, we report a new class of cyclodextrin (CyD) derivatives rationally designed to improve the Aβ recognition and to modulate its aggregation. In particular, a dimethylamino aromatic moiety was conjugated to βCyD or γCyD to explore how different structural aspects of these derivatives could influence the recognition and the aggregation of Aβ. The conjugation of the Aβ recognition moiety to CyDs resulted in a significant suppression of the self‐assembly propensity of Aβ when the dimethylamino aromatic moiety was attached to the upper rim of βCyD. The activity of the derivatives toward Aβ confirms that the conjugation of CyDs with Aβ recognition moieties may be considered a promising approach for designing new molecules that interfere with Aβ aggregation.