Design, synthesis, and biological evaluation of glycine-based molecular tongs as inhibitors of Abeta1-40 aggregation in vitro

Bioorganic & Medicinal Chemistry
Saverio CellamareAngelo Carotti

Abstract

A series of N-terminus benzamides of glycine-based symmetric peptides, linked to m-xylylenediamine and 3,4'-oxydianiline spacers, were prepared and tested as inhibitors of beta-amyloid peptide Abeta(1-40) aggregation in vitro. Compounds with good anti-aggregating activity were detected. Polyphenolic amides showed the highest anti-aggregating activity, with IC(50) values in the micromolar range. Structure-activity relationships suggested that pi-pi stacking and hydrogen-bonding interactions play a key role in the inhibition of Abeta(1-40) self-assembly leading to amyloid fibrils.

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Citations

Nov 25, 2011·Journal of Medicinal Chemistry·Raffaella Zoe PellicaniNicola Antonio Colabufo
Mar 3, 2015·Journal of Biomolecular Structure & Dynamics·Dhawal Shah, Abdul Rajjak Shaikh
Nov 30, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Isabella BologninoMarco Catto
Jun 29, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rosa PurgatorioMarco Catto
Jan 16, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Alisa A NevskayaCosimo D Altomare

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