Journal Article

FZJ-2015-03605

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation

Chiriano, G. ; De Simone, A. ; Mancini, F. ; Perez, D. I. ; Cavalli, A. ; Bolognesi, M. L. ; Legname, G. ; Martinez, A. ; Andrisano, V. ; Carloni, P.FZJ* ; Roberti, M. (Corresponding Author)

2012
Elsevier Science Amsterdam [u.a.]

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Please use a persistent id in citations: doi:10.1016/j.ejmech.2011.12.016

Abstract: In 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.

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Contributing Institute(s):

1. GRS (GRS)
2. Computational Biomedicine (IAS-5)

Research Program(s):

1. 899 - ohne Topic (POF2-899) (POF2-899)

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Database coverage:
; BIOSIS Previews ; Current Contents - Life Sciences ; IF < 5 ; JCR ; NCBI Molecular Biology Database ; SCOPUS ; Science Citation Index ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection

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