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.
G. P. Chiriano, A. De Simone, F. Mancini, D. I. Perez, A. Cavalli, M. L. Bolognesi, et al. (2012). A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: structure-based design, synthesis, and biological evaluation. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 48, 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
DE SIMONE, ANGELA;MANCINI, FRANCESCA;CAVALLI, ANDREA;BOLOGNESI, MARIA LAURA;ANDRISANO, VINCENZA;ROBERTI, MARINELLA
2012
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
