Disubstituted Bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors
Hohlfeld, Konrad, Tomassi, Cyrille, Wegner, Jörg Kurt, Kesteleyn, Bart and Linclau, Bruno (2011) Disubstituted Bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors. ACS Medicinal Chemistry Letters, 2, (6), 461-465. (doi:10.1021/ml2000356).
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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
|Subjects:||Q Science > QD Chemistry|
|Divisions:||University Structure - Pre August 2011 > School of Chemistry
|Date Deposited:||10 Jun 2011 07:35|
|Last Modified:||02 Mar 2012 13:38|
|Contributors:||Hohlfeld, Konrad (Author)
Tomassi, Cyrille (Author)
Wegner, Jörg Kurt (Author)
Kesteleyn, Bart (Author)
Linclau, Bruno (Author)
|RDF:||RDF+N-Triples, RDF+N3, RDF+XML, Browse.|
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