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P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Sep 20; Vol. 14 (18), pp. 4651-4. - Publication Year :
- 2004
-
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.
- Subjects :
- Cell Line, Tumor
Drug Resistance, Multiple, Viral
HIV Protease Inhibitors chemical synthesis
HIV Protease Inhibitors pharmacology
HIV-1 enzymology
HIV-1 isolation & purification
Humans
Indinavir analogs & derivatives
Indinavir chemical synthesis
Indinavir chemistry
Indinavir pharmacology
Oxadiazoles chemical synthesis
Oxadiazoles pharmacology
Pyridines chemistry
Stereoisomerism
HIV Protease Inhibitors chemistry
HIV-1 drug effects
Oxadiazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 14
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15324882
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.06.092