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 microM) and antiviral activity in cell culture (EC50 = 0.96 microM, SI = 65.69).
Lee
Y S
YS
Division of Life Sciences, Korea Institute of Science & Technology, Cheongryang, Seoul, South Korea.
Lee
Y S
YS
Lee
J Y
JY
Kim
S N
SN
Lee
C K
CK
Park
H
H
D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D002478:Cells, Cultured; D004147:Dioxins / Q000737:chemistry / Q000494:pharmacology*; D017320:HIV Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests
D019380:Anti-HIV Agents; D004147:Dioxins; D017320:HIV Protease Inhibitors