WFIGR ID=ol990586yn00001> |
A series of simple heterocyclic HIV-1 protease inhibitors
were developed on the basis of size, shape, and electronic complementarity to theactive site of the enzyme. The
C2-symmetric heterocycles do not contain a transition-state isostere nor are they active site directed irreversibleinhibitors; thus, they represent the success of a ne
w design strategy. The first generation heterocycles inhibit the protease in the micromolarrange,
whereas control compounds sho
w no bioactivity at the same concentrations.
