6-Hydroxy-1,3-dioxin-4-ones as non-peptidic HIV protease inhibitors

HIV protease inhibitors containing 6-hydroxy-1,3-dioxin-4-one ring system as a new scaffold have been prepared. Among them, compound 4d showed potent HIV protease inhibitory activity (IC50=0.01 μM) and antiviral activity in cell culture (EC50=0.96 μM, SI=65.69).