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

Academic Article
Publication Date:
2001
abstract:
We describe the asymmetric total synthesis of a trifluoromethyl (Tfm) analogue of the aspartate protease inhibitor pepstatin incorporating two gamma-Tfm-gamma-amino-beta-hydroxybutyric acid (gamma-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) © 2001 Elsevier Science Ltd. All rights reserved.
Iris type:
01.01 Articolo in rivista
Keywords:
Asymmetric synthesis; HIV; Metalloproteinase; Peptide isosteres; Trifluoromethyl group
List of contributors:
Handle:
https://iris.cnr.it/handle/20.500.14243/279271
Published in:
TETRAHEDRON (OXF., PRINT)
Journal