Title of article
Total synthesis of a pepstatin analog incorporating two trifluoromethyl hydroxymethylene isosteres (Tfm-GABOB) and evaluation of Tfm-GABOB containing peptides as inhibitors of HIV-1 protease and MMP-9
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 ,
Issue Information
هفته نامه با شماره پیاپی سال 2001
Pages
12
From page
6511
To page
6522
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
Journal title
Tetrahedron
Serial Year
2001
Journal title
Tetrahedron
Record number
1082257
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