Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.
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.
Mesh Terms:
Clinical Trials as Topic, Crystallography, X-Ray, Drug Design, Drug Resistance, Viral, HIV Infections, HIV Protease Inhibitors, HIV-1, Humans, Ligands, Molecular Structure, Structure-Activity Relationship, Sulfonamides
Clinical Trials as Topic, Crystallography, X-Ray, Drug Design, Drug Resistance, Viral, HIV Infections, HIV Protease Inhibitors, HIV-1, Humans, Ligands, Molecular Structure, Structure-Activity Relationship, Sulfonamides
Bioorg. Med. Chem.
Date: Dec. 15, 2007
PubMed ID: 17900913
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