Disubstituted bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors (II)

Hohlfeld, Konrad, Wegner, Jörg Kurt, Kesteleyn, Bart, Linclau, Bruno and Unge, Johan (2015) Disubstituted bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors (II). Journal of Medicinal Chemistry, 58 (9), 4029-4038. (doi:10.1021/acs.jmedchem.5b00358).

Record type: Article

Abstract

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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Published date: 30 April 2015

Additional Information: This document is the unedited Author’s version of a Submitted Work that was subsequently accepted for publication in [JournalTitle], copyright © American Chemical Society after peer review.

Organisations: Organic Chemistry: Synthesis, Catalysis and Flow