A series of nonsymmetrically substituted cyclic ureacarboxamides was s
ynthesized and evaluated for antiviral activity as a function of the i
nhibition of HIV-protease. Selected protease inhibitors were also eval
uated for oral bioavailability. The synthesis, pharmacology, quantitat
ive structure-activity relationship (QSAR), and pharmacokinetics for t
he series will be discussed.