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

@article{Cellamare2008DesignSA,
  title={Design, synthesis, and biological evaluation of glycine-based molecular tongs as inhibitors of Abeta1-40 aggregation in vitro.},
  author={Saverio Cellamare and Angela Stefanachi and Diana Antonella Stolfa and Teodora Basile and Marco Catto and Francesco Campagna and Eddy Sotelo and Pasquale Acquafredda and Angelo Carotti},
  journal={Bioorganic & medicinal chemistry},
  year={2008},
  volume={16 9},
  pages={4810-22}
}
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… CONTINUE READING
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