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Bioorg Med Chem Lett. 2004 Sep 20;14(18):4651-4.

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

Author information

1
Department of Basic Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. ron_kim@merck.com

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.

PMID:
15324882
DOI:
10.1016/j.bmcl.2004.06.092
[Indexed for MEDLINE]

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