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Bioorg Med Chem. 2007 Dec 15;15(24):7576-80. Epub 2007 Sep 14.

Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.

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  • 1Departments of Chemistry and Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.

Abstract

Our structure-based design strategies which specifically target the HIV-1 protease backbone, resulted in a number of exceedingly potent nonpeptidyl inhibitors. One of these inhibitors, darunavir (TMC114), contains a privileged, structure-based designed high-affinity P2 ligand, 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane (bis-THF). Darunavir has recently been approved for the treatment of HIV/AIDS patients harboring multidrug-resistant HIV-1 variants that do not respond to previously existing HAART regimens.

PMID:
17900913
[PubMed - indexed for MEDLINE]
PMCID:
PMC2112938
Free PMC Article
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