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

Disubstituted bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors (II)
Disubstituted bis-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors (II)
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
0022-2623
4029-4038
Hohlfeld, Konrad
f40f3c74-b8b2-4951-bacb-ae7a4841e20b
Wegner, Jörg Kurt
36196faf-a073-4c4c-9e0e-92733c17e68a
Kesteleyn, Bart
324c1b14-2540-4223-859c-89a21f9e5dec
Linclau, Bruno
19b9cacd-b8e8-4c65-af36-6352cade84ba
Unge, Johan
a30ba536-a5ae-45ba-8d77-cef44f35169b
Hohlfeld, Konrad
f40f3c74-b8b2-4951-bacb-ae7a4841e20b
Wegner, Jörg Kurt
36196faf-a073-4c4c-9e0e-92733c17e68a
Kesteleyn, Bart
324c1b14-2540-4223-859c-89a21f9e5dec
Linclau, Bruno
19b9cacd-b8e8-4c65-af36-6352cade84ba
Unge, Johan
a30ba536-a5ae-45ba-8d77-cef44f35169b

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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More information

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

Identifiers

Local EPrints ID: 381203
URI: https://eprints.soton.ac.uk/id/eprint/381203
ISSN: 0022-2623
PURE UUID: 29c663c9-d53e-48e7-8657-66f2f348a2bb
ORCID for Bruno Linclau: ORCID iD orcid.org/0000-0001-8762-0170

Catalogue record

Date deposited: 28 Sep 2015 12:27
Last modified: 20 Jul 2019 01:07

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