THE DESIGN AND SYNTHESIS OF NOVEL HYDROXYPROLINE INHIBITORS OF HIV-1 PROTEINASE

Authors
HOLMES DS BETHELL RC HANN MM KITCHIN J STARKEY ID STORER R
Citation
Ds. Holmes et al., THE DESIGN AND SYNTHESIS OF NOVEL HYDROXYPROLINE INHIBITORS OF HIV-1 PROTEINASE, Bioorganic & medicinal chemistry letters, 3(8), 1993, pp. 1485-1491
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
8
Year of publication
1993
Pages
1485 - 1491
Database
ISI
SICI code
0960-894X(1993)3:8<1485:TDASON>2.0.ZU;2-O
Abstract
The synthesis and activity of novel hydroxyproline inhibitors of HIV-1 proteinase is described. Compound (R)-4 was a potent inhibitor, IC50 = 0.07 muM, however it is likely that the thiazolidine moiety rather t han the novel hydroxyproline group is the primary determinant of bindi ng.