Disubstituted bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors (II)
A series of darunavir analogues featuring a substituted bis-THF ring as P2 ligand have been synthesized and evaluated. Very 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 mu...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
2015-04-30.
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| Subjects: | |
| Online Access: | Get fulltext |
| Summary: | A series of darunavir analogues featuring a substituted bis-THF ring as P2 ligand have been synthesized and evaluated. Very 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. Crystal structure analysis was conducted on a number of PI analogues in complex with HIV-1 protease |
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