Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue -, Pages 206-213Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.12.016
Keywords
Alzheimer's disease; Amyloid-beta peptide; Drug design; Hit identification; 2-Aminoimidazole
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Funding
- Italian Institute of Technology (IIT)
- University of Bologna
- CSIC
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In this work, we report a rational structure-based approach aimed at the discovery of new 2-aminoimidazoles as beta-secretase inhibitors. Taking advantage of a microwave-assisted synthetic protocol, a small library of derivatives was obtained and biologically evaluated. Two compounds showed promising activities in both enzymatic and cellular assays. Moreover, one of them exhibited the capability to cross the blood brain barrier as assessed by the parallel artificial membrane permeability assay. (C) 2011 Elsevier Masson SAS. All rights reserved.
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