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.
Bioorganic & Medicinal Chemistry Letters
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.
complete list of authors
Thompson, Scott K||Eppley, Alecia M||Frazee, James S||Darcy, Michael G||Lum, Robert T||Tomaszek, Thaddeus A||Ivanoff, Lucinda A||Morris, Jane F||Sternberg, Edmund J||Lambert, Dennis M||Fernandez, Annabellee V||Petteway, Stephen R||Meek, Thomas D||Metcalf, Brian W||Gleason, John G