期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 48, 期 -, 页码 206-213出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.12.016
关键词
Alzheimer's disease; Amyloid-beta peptide; Drug design; Hit identification; 2-Aminoimidazole
资金
- Italian Institute of Technology (IIT)
- University of Bologna
- CSIC
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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