Disubstituted Bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors
Disubstituted Bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors
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
461-465
Hohlfeld, Konrad
f40f3c74-b8b2-4951-bacb-ae7a4841e20b
Tomassi, Cyrille
51fbf42e-4b91-481c-8528-95ca06e30c40
Wegner, Jörg Kurt
40bd80aa-3940-41f8-8d1a-3d3181f04ae7
Kesteleyn, Bart
324c1b14-2540-4223-859c-89a21f9e5dec
Linclau, Bruno
19b9cacd-b8e8-4c65-af36-6352cade84ba
March 2011
Hohlfeld, Konrad
f40f3c74-b8b2-4951-bacb-ae7a4841e20b
Tomassi, Cyrille
51fbf42e-4b91-481c-8528-95ca06e30c40
Wegner, Jörg Kurt
40bd80aa-3940-41f8-8d1a-3d3181f04ae7
Kesteleyn, Bart
324c1b14-2540-4223-859c-89a21f9e5dec
Linclau, Bruno
19b9cacd-b8e8-4c65-af36-6352cade84ba
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), .
(doi:10.1021/ml2000356).
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
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Published date: March 2011
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Local EPrints ID: 190077
URI: http://eprints.soton.ac.uk/id/eprint/190077
ISSN: 1948-5875
PURE UUID: cf7d8dc5-677d-4583-bb28-f0a27bd1f7f6
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Date deposited: 10 Jun 2011 07:35
Last modified: 15 Mar 2024 03:05
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Author:
Konrad Hohlfeld
Author:
Cyrille Tomassi
Author:
Jörg Kurt Wegner
Author:
Bart Kesteleyn
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