Article
Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor.
Bioorganic & medicinal chemistry - 1 Dec 1999
Prasad J V, Boyer F E, Domagala J M, Ellsworth E L, Gajda C, Hamilton H W, Hagen S E, Markoski L J, Steinbaugh B A, Tait B D, Humblet C, Lunney E A, Pavlovsky A, Rubin J R, Ferguson D, Graham N, Holler T, Hupe D, Nouhan C, Tummino P J, Urumov A, Zeikus E, Zeikus G, Gracheck S J, Erickson J W
Abstract excerpt
With the insight generated by the availability of X-ray crystal structures of various 5,6-dihydropyran-2-ones bound to HIV PR, inhibitors possessing various alkyl groups at the 6-position of 5,6-dihydropyran-2-one ring were synthesized. The inhibitors possessing a 6-alkyl group exhibited superior...
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