Synthesis and antiviral activity of a novel class of HIV-1 protease inhibitors containing a heterocyclic P1-P2 amide bond isostere Academic Article uri icon


  • 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.

published proceedings

  • Bioorganic & Medicinal Chemistry Letters

altmetric score

  • 3

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.

citation count

  • 42

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

publication date

  • January 1994