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

作者信息

Cellamare Saverio, Stefanachi Angela, Stolfa Diana A, Basile Teodora, Catto Marco, Campagna Francesco, Sotelo Eddy, Acquafredda Pasquale, Carotti Angelo

机构信息

Dipartimento Farmaco-chimico, Università degli Studi di Bari, Via Orabona 4, 70125 Bari, Italy.

出版信息

Bioorg Med Chem. 2008 May 1;16(9):4810-22. doi: 10.1016/j.bmc.2008.03.052. Epub 2008 Mar 25.

DOI:10.1016/j.bmc.2008.03.052
PMID:18406152
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.

摘要

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