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

Abstract

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 (IC(50) = 0.01 muM) and antiviral activity in cell culture (EC(50) = 0.96 muM, SI = 65.69). (C) 2000 Elsevier Science Ltd. All rights reserved.