BENEFICIAL REPLACEMENT OF THE P-1 PHENYLALANINE SIDE-CHAIN IN HIV-1 PROTEASE INHIBITORS OF THE DIFLUOROSTATONE TYPE

Authors
SCHIRLIN D VANDORSSELAER V TARNUS C TAYLOR DL TYMS AS BALTZER S WEBER F REMY JM BRENNAN T FARR R JANOWICK D
Citation
D. Schirlin et al., BENEFICIAL REPLACEMENT OF THE P-1 PHENYLALANINE SIDE-CHAIN IN HIV-1 PROTEASE INHIBITORS OF THE DIFLUOROSTATONE TYPE, Bioorganic & medicinal chemistry letters, 4(2), 1994, pp. 241-246
Citations number
15
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
2
Year of publication
1994
Pages
241 - 246
Database
ISI
SICI code
0960-894X(1994)4:2<241:BROTPP>2.0.ZU;2-G
Abstract
An O-benzyltyrosyl P-1 side chain on HIV-1 protease inhibitors of the difluorostatone type confers increased potency and an improved cytotox ic index in infected cells. A number of carboxy or amino termini modif ications are permitted for instance, carboxy termini tertiary amides.