597563-62-7Relevant academic research and scientific papers
HIV protease inhibitors with picomolar potency against PI-resistant HIV-1 by extension of the P3 substituent
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.
, p. 2569 - 2572 (2007/10/03)
A biaryl pyridylfuran P3 substituent on the hydroxyethylene isostere scaffold affords HIV protease inhibitors (PI's) with picomolar (IC50) 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 t1/2 of indinavir. Inhibition of multiple P450 isoforms is dependent on the regiochemistry of the pyridyl nitrogen in these compounds.
