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.
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, Di; Cavalli, A; Bolognesi, Ml; Legname, Giuseppe; Martinez, A; Andrisano, V; Carloni, P; Roberti, M.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 48:February(2012), pp. 206-213. [10.1016/j.ejmech.2011.12.016]
A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
Legname, Giuseppe;
2012-01-01
Abstract
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.| File | Dimensione | Formato | |
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