SYNTHESIS AND ANTIVIRAL ACTIVITY OF A NOVEL CLASS OF HIV-1 PROTEASE INHIBITORS CONTAINING A HETEROCYCLIC P-1'-P-2' AMIDE BOND ISOSTERE

Citation
Sk. Thompson et al., SYNTHESIS AND ANTIVIRAL ACTIVITY OF A NOVEL CLASS OF HIV-1 PROTEASE INHIBITORS CONTAINING A HETEROCYCLIC P-1'-P-2' AMIDE BOND ISOSTERE, Bioorganic & medicinal chemistry letters, 4(20), 1994, pp. 2441-2446
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
4
Issue
20
Year of publication
1994
Pages
2441 - 2446
Database
ISI
SICI code
0960-894X(1994)4:20<2441:SAAAOA>2.0.ZU;2-9
Abstract
A novel series of hydroxyethylene-based peptidomimetics that contain 2 -substituted nitrogen heterocycles as P-1'-P-2' amide bond isosteres h as been prepared and evaluated as inhibitors of HIV-1 protease and in vitro HIV-1 replication. Many of these compounds exhibit inhibition co nstants in the low to subnanomolar range. Structure-activity relations hips are discussed.