In this work, we report a rational structure-based approach aimed at the discovery of new 2- aminoimidazoles as b-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 capa- bility to cross the bloodebrain barrier as assessed by the parallel arti␣cial membrane permeability assay.
|Titolo:||A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation|
|Autori:||CHIRIANO G; DE SIMONE A; MANCINI F; PEREZ DI; CAVALLI A; BOLOGNESI ML; LEGNAME G; MARTINEZ A; ANDRISANO V; CARLONI P; ROBERTI M|
|Rivista:||EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY|
|Data di pubblicazione:||2012|
|Digital Object Identifier (DOI):||10.1016/j.ejmech.2011.12.016|
|Appare nelle tipologie:||1.1 Journal article|