DIFUNCTIONAL ENOLS OF N-PROTECTED AMINO-ACIDS AS LOW-MOLECULAR-WEIGHTAND NOVEL INHIBITORS OF HIV-1 PROTEASE

Authors
VAILLANCOURT M VANASSE B COHEN E SAUVE G
Citation
M. Vaillancourt et al., DIFUNCTIONAL ENOLS OF N-PROTECTED AMINO-ACIDS AS LOW-MOLECULAR-WEIGHTAND NOVEL INHIBITORS OF HIV-1 PROTEASE, Bioorganic & medicinal chemistry letters, 3(6), 1993, pp. 1169-1174
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
6
Year of publication
1993
Pages
1169 - 1174
Database
ISI
SICI code
0960-894X(1993)3:6<1169:DEONAA>2.0.ZU;2-S
Abstract
The synthesis of difunctional enols of simple amino acids and their no vel inhibitory activity against human immunodeficiency virus type 1 pr otease (HIV-PR) are described. By modifying the substituents on these enols, we were able to achieve mid-nanomolar range in activity against HIV-1 protease which is, to our knowledge, the best reported activity for molecules that do not contain at least one peptide linkage.