757247-09-9Relevant academic research and scientific papers
P1′ oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1
Kim, Ronald M.,Rouse, Elizabeth A.,Chapman, Kevin T.,Schleif, William A.,Olsen, David B.,Stahlhut, Mark,Rutkowski, Carrie A.,Emini, Emilio A.,Tata, James R.
, p. 4651 - 4654 (2004)
HIV-1 protease inhibitors bearing 1,3,4-oxadiazoles at the P1′ position are highly active against native and PI-resistant HIV-1. HIV-1 protease inhibitors (PI's) bearing 1,3,4-oxadiazoles at the P1′ position were prepared by a novel method involving the diastereoselective installation of a carboxylic acid and conversion to the P1′ heterocycle. The compounds are picomolar inhibitors of native HIV-1 protease, with most of the compounds maintaining excellent antiviral activity against a panel of PI-resistant strains.
