A series of darunavir analogues featuring a substituted bis-THF ring as P2 ligand have been synthesized and evaluated. High affinity protease inhibitors (PIs) with an interesting activity on wild-type HIV and a panel of multi-PI resistant HIV-1 mutants containing clinically observed, primary mutations were identified using a cell-based assay. A number of PIs have been synthesized that show equivalent and greater activity for HIV-1 mutant strains as compared to wild-type HIV-1. The activity on the purified enzyme was confirmed for a selection of analogues. © 2011 American Chemical Society.
CITATION STYLE
Hohlfeld, K., Tomassi, C., Wegner, J. K., Kesteleyn, B., & Linclau, B. (2011). Disubstituted bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors. ACS Medicinal Chemistry Letters, 2(6), 461–465. https://doi.org/10.1021/ml2000356
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