Document Report Card
Basic Information
ID: ALA1134901
Journal: Bioorg Med Chem Lett
Title: Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.
Authors: Duffy JL, Kevin NJ, Kirk BA, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Kuo LC, Jin L, Lin JH, Emini EA, Tata JR.
Abstract: Substitution of the t-butylcarboxamide substituent in analogues of the HIV protease inhibitor (PI) Indinavir with a trifluoroethylamide moiety confers greater potency against both the wild-type (NL4-3) virus and PI-resistant HIV. The trifluoroethyl substituent also affords a slower clearance rate in vivo (dogs); however, this may be due to more potent inhibition of at least two P450 isoforms.
CiteXplore: 12161148