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Article

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

Journal of medicinal chemistry - 14 May 2015

Hohlfeld Konrad, Wegner Jörg Kurt, Kesteleyn Bart, Linclau Bruno, Unge Johan

Abstract excerpt

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...

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Identifiers

PMID: 25897791
DOI: 10.1021/acs.jmedchem.5b00358

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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