A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
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 a...
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Personal Name(s): | Chiriano, Gianpaolo |
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De Simone, Angela / Mancini, Francesca / Perez, Daniel I. / Cavalli, Andrea / Bolognesi, Maria Laura / Legname, Giuseppe / Martinez, Ana / Andrisano, Vincenza / Carloni, Paolo / Roberti, Marinella (Corresponding Author) | |
Contributing Institute: |
Computational Biomedicine; IAS-5 GRS; GRS |
Published in: | European journal of medicinal chemistry, 48 (2012) S. 206 - 213 |
Imprint: |
Amsterdam [u.a.]
Elsevier Science
2012
|
DOI: |
10.1016/j.ejmech.2011.12.016 |
Document Type: |
Journal Article |
Research Program: |
ohne Topic |
Publikationsportal JuSER |
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. |