Detalle de: A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
| Title | A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation |
| 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. |
| Apa Reference | Chiriano, G., De Simone, A., Mancini, F., Perez, D. I., Cavalli, A., Bolognesi, M. L., Legname, G., Martinez, A., Andrisano, V., Carloni, P., & Roberti, M. (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 |
| Doi | 10.1016/j.ejmech.2011.12.016 |
| Publication Date | Feb 2012 |
| Publication Type | Article |
| Researcher | Ana Martínez |
| Ontology | Drug Discovery and design |
| Research Groups | Translational Medicinal and Biological Chemistry |
| Tools |