P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1 |
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| Authors: | 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 |
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| Affiliation: | Department of Basic Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. ron_kim@merck.com |
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| 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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