Synthesis and antiviral activity of a novel class of HIV-1 protease inhibitors containing a heterocyclic P1′-P2′ amide bond isostere
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A novel series of hydroxyethylene-based peptidomimetics that contain 2-substituted nitrogen heterocycles as P 1 ′-P 2 ′ amide bond isosteres has been prepared and evaluated as inhibitors of HIV-1 protease and in vitro HIV-1 replication. Many of these compounds exhibit inhibition constants in the low to subnanomolar range. Structure-activity relationships are discussed. © 1994.
author list (cited authors)
Thompson, S. K., Eppley, A. M., Frazee, J. S., Darcy, M. G., Lum, R. T., Tomaszek, T. A., ... Gleason, J. G.