Probing Multidrug-Resistance and Protein–Ligand Interactions with Oxatricyclic Designed Ligands in HIV-1 Protease Inhibitors
Written by Arun K. Ghosh on November 8, 2010 – 5:00 am -A healthier HAART: We report the design, synthesis, biological evaluation, and X-ray crystallographic analysis of a new class of HIV-1 protease inhibitors. Compound 4 proved to be an extremely potent inhibitor toward various multidrug-resistant HIV-1 variants, representing a near 10-fold improvement over darunavir (DRV). Compound 4 also blocked protease dimerization with at least 10-fold greater potency than DRV.
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