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Comparative Study
. 2004 Sep 20;14(18):4651-4.
doi: 10.1016/j.bmcl.2004.06.092.

P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1

Ronald M Kim  1 , Elizabeth A Rouse, Kevin T Chapman, William A Schleif, David B Olsen, Mark Stahlhut, Carrie A Rutkowski, Emilio A Emini, James R Tata
Affiliations
Comparative Study

P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1

Ronald M Kim et al. Bioorg Med Chem Lett. .

Abstract

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.

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