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

Arun K Ghosh, Zachary L Dawson, Hiroaki Mitsuya

Bioorganic & medicinal chemistry 2007 Dec 15

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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.

Citation

Arun K Ghosh, Zachary L Dawson, Hiroaki Mitsuya. Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV. Bioorganic & medicinal chemistry. 2007 Dec 15;15(24):7576-80