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A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation

AuthorsChiriano, G.; De Simone, A.; Mancini, F.; Perez, D.I.; Cavalli, A.; Bolognesi, Maria Laura; Legname, G.; Martinez, A. ; Andrisano, Vincenza; Carloni, P.; Roberti, M.
Issue Date2012
CitationEuropean Journal of Medicinal Chemistry 48: 206- 213 (2012)
AbstractIn this work, we report a rational structure-based approach aimed at the discovery of new 2-aminoimidazoles as β-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. © 2011 Elsevier Ltd. All rights reserved.
Identifiersdoi: 10.1016/j.ejmech.2011.12.016
issn: 0223-5234
Appears in Collections:(IQM) Artículos
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