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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Description/Abstract
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
| Item Type: | Article |
|---|---|
| ISSNs: | 1948-5875 (print) 1948-5875 (electronic) |
| Subjects: | Q Science > QD Chemistry |
| Divisions: | University Structure - Pre August 2011 > School of Chemistry |
| Item ID: | 190077 |
| 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) |
| Date: | March 2011 |
| Status: | Published |
| URI: | http://eprints.soton.ac.uk/id/eprint/190077 |
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