TY  - JOUR
AU  - Chiriano, Gianpaolo
AU  - De Simone, Angela
AU  - Mancini, Francesca
AU  - Perez, Daniel I.
AU  - Cavalli, Andrea
AU  - Bolognesi, Maria Laura
AU  - Legname, Giuseppe
AU  - Martinez, Ana
AU  - Andrisano, Vincenza
AU  - Carloni, Paolo
AU  - Roberti, Marinella
TI  - A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
JO  - European journal of medicinal chemistry
VL  - 48
SN  - 0223-5234
CY  - Amsterdam [u.a.]
PB  - Elsevier Science
M1  - FZJ-2015-03605
SP  - 206 - 213
PY  - 2012
AB  - 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.
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000300484900022
DO  - DOI:10.1016/j.ejmech.2011.12.016
UR  - https://juser.fz-juelich.de/record/201300
ER  -