NOVEL PSEUDOSYMMETRIC INHIBITORS OF HIV-1 PROTEASE

Authors
FASSLER A ROSEL J GRUTTER M TINTELNOTBLOMLEY M ALTERI E BOLD G LANG M
Citation
A. Fassler et al., NOVEL PSEUDOSYMMETRIC INHIBITORS OF HIV-1 PROTEASE, Bioorganic & medicinal chemistry letters, 3(12), 1993, pp. 2837-2842
Citations number
41
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
12
Year of publication
1993
Pages
2837 - 2842
Database
ISI
SICI code
0960-894X(1993)3:12<2837:NPIOHP>2.0.ZU;2-J
Abstract
Compounds containing the easily accessible Phe[CH(OH)CH2N(NH)]Phe dipe ptide isostere as a non-hydrolyzable replacement of the scissile amide bond in the natural substrate are potent inhibitors of HIV-1 protease . The expected symmetric binding pattern of the most potent inhibitor in this series (CGP 53820, IC50 = 9 nM) is illustrated by the X-ray an alysis performed with the corresponding enzyme-inhibitor complex.