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
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.