Author/Authors :
Cristina Pesenti، نويسنده , , Alberto Arnone، نويسنده , , Stefano Bellosta، نويسنده , , Pierfrancesco Bravo، نويسنده , , Monica Canavesi، نويسنده , , Eleonora Corradi، نويسنده , , Massimo Frigerio، نويسنده , , Stefano V Meille، نويسنده , , Mara Monetti، نويسنده , , Walter Panzeri، نويسنده , , Fiorenza Viani، نويسنده , , Romina Venturini، نويسنده , , Matteo Zanda، نويسنده ,
Abstract :
We describe the asymmetric total synthesis of a trifluoromethyl (Tfm) analogue of the aspartate protease inhibitor pepstatin incorporating two γ-Tfm-γ-amino-β-hydroxybutyric acid (γ-Tfm-GABOB) units instead of the natural statine units. The title compound as well as several Tfm-substituted precursors were tested as inhibitors of HIV-1 protease and Gelatinase B (MMP-9)
Keywords :
Asymmetric synthesis , peptide isosteres , HIV , metalloproteinase , trifluoromethyl group
