Article
4-Hydroxy-5,6-dihydropyrones as inhibitors of HIV protease: the effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters.
Journal of medicinal chemistry - 5 Jul 2001
Hagen S E, Domagala J, Gajda C, Lovdahl M, Tait B D, Wise E, Holler T, Hupe D, Nouhan C, Urumov A, Zeikus G, Zeikus E, Lunney E A, Pavlovsky A, Gracheck S J, Saunders J, VanderRoest S, Brodfuehrer J
Abstract excerpt
Due largely to the emergence of multi-drug-resistant HIV strains, the development of new HIV protease inhibitors remains a high priority for the pharmaceutical industry. Toward this end, we previously identified a 4-hydroxy-5,6-dihydropyrone lead compound (CI-1029, 1) which possesses excellent activity against the protease enzyme, good antiviral efficacy in cellular assays, and promising bioavailability in...
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