Article
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.
Bioorganic & medicinal chemistry letters - 4 Aug 2003
Duffy Joseph L, Rano Thomas A, Kevin Nancy J, Chapman Kevin T, Schleif William A, Olsen David B, Stahlhut Mark, Rutkowski Carrie A, Kuo Lawrence C, Jin Lixia, Lin Jiunn H, Emini Emilio A, Tata James R
Abstract excerpt
A biaryl pyridylfuran P(3) substituent on the hydroxyethylene isostere scaffold affords HIV protease inhibitors (PI's) with picomolar (IC(50)) potency against the protease enzymes from PI-resistant HIV-1 strains. Inclusion of a gem-dimethyl substituent afforded compound 3 with 100% oral bioavailability (dogs) and more than double the t(1/2) of indinavir. Inhibition of multiple P450 isoforms is dependent on the...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.