4-Hydroxy-5, 6-dihydropyrones as inhibitors of HIV protease: the effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters

…, C Nouhan, A Urumov, G Zeikus, E Zeikus…

文献索引：Hagen; Domagala; Gajda; Lovdahl; Tait; Wise; Holler; Hupe; Nouhan; Urumov; Zeikus; Lunney; Pavlovsky; Gracheck; Saunders; VanderRoest; Brodfuehrer Journal of Medicinal Chemistry, 2001 , vol. 44, # 14 p. 2319 - 2332

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被引用次数: 53

摘要

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 several animal species. The search for a ...