Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
A series of nonsymmetrically substituted cyclic ureacarboxamides was synthesized and evaluated for antiviral activity as a function of the inhibition of HIV-protease. Selected protease inhibitors were also evaluated for oral bioavailability. The synthesis, pharmacology, quantitative structure-activity relationship (QSAR), and pharmacokinetics for the series will be discussed.
Wilkerson
W W
WW
DuPont Merck Pharmaceutical Company, Experimental Station, Wilmington, Delaware 19880-0500, USA.
Dax
S
S
Cheatham
W W
WW
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D012367:RNA, Viral / Q000032:analysis; D013329:Structure-Activity Relationship; D014508:Urea / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
D019380:Anti-HIV Agents; D017320:HIV Protease Inhibitors; D012367:RNA, Viral; D014508:Urea