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Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors (II)

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Author

  • Konrad Hohlfeld
  • Joerg Kurt Wegner
  • Bart Kesteleyn
  • Bruno Linclau
  • Johan Unge

Summary, in English

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.

Department/s

Publishing year

2015

Language

English

Pages

4029-4038

Publication/Series

Journal of Medicinal Chemistry

Volume

58

Issue

9

Document type

Journal article

Publisher

The American Chemical Society (ACS)

Topic

  • Medicinal Chemistry

Status

Published

ISBN/ISSN/Other

  • ISSN: 1520-4804