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Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors.

dc.rights.licenseopenen_US
dc.contributor.authorSUCHAUD, Virginie
dc.contributor.authorBAILLY, Fabrice
dc.contributor.authorLION, Cedric
hal.structure.identifierMicrobiologie Fondamentale et Pathogénicité [MFP]
dc.contributor.authorCALMELS, Christina
hal.structure.identifierMicrobiologie Fondamentale et Pathogénicité [MFP]
dc.contributor.authorANDRÉOLA, Marie-Line
dc.contributor.authorCHRIST, Frauke
dc.contributor.authorDEBYSER, Zeger
dc.contributor.authorCOTELLE, Philippe
dc.date.accessioned2024-11-15T13:23:49Z
dc.date.available2024-11-15T13:23:49Z
dc.date.issued2014-06-12
dc.identifier.issn1520-4804en_US
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/203310
dc.description.abstractEnWe report herein further insight into the biological activities displayed by a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs). Substitution of the N-hydroxyimide two-metal binding pharmacophore at position 4 by carboxamido side chains was previously shown by us to be fruitful for this scaffold, since strong human immunodeficiency virus type 1 integrase (HIV-1 IN) inhibitors in the low nanomolar range associated with low micromolar anti-HIV activities were obtained. We investigated the influence of substitution at position 7 on biological activity. Introduction of electron-withdrawing functional groups such as the nitro moiety at position 7 led to a noticeable improvement of antiviral activity, down to low nanomolar anti-HIV potencies, with advantageous therapeutic indexes going close to those of the clinically used raltegravir and retained potencies against a panel of IN mutants.
dc.language.isoENen_US
dc.subject.enAryl Hydrocarbon Hydroxylases
dc.subject.enCell Line
dc.subject.enTumor
dc.subject.enCytochrome P-450 CYP2C9
dc.subject.enCytochrome P-450 CYP3A
dc.subject.enCytochrome P-450 CYP3A Inhibitors
dc.subject.enDrug Resistance
dc.subject.enViral
dc.subject.enHIV Integrase Inhibitors
dc.subject.enHIV-1
dc.subject.enHumans
dc.subject.enIsoquinolines
dc.subject.enMolecular Docking Simulation
dc.subject.enMutation
dc.subject.enStructure-Activity Relationship
dc.title.enInvestigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors.
dc.title.alternativeJ Med Chemen_US
dc.typeArticle de revueen_US
dc.identifier.doi10.1021/jm500109zen_US
dc.subject.halSciences du Vivant [q-bio]/Microbiologie et Parasitologieen_US
dc.identifier.pubmed24793360en_US
bordeaux.journalJournal of Medicinal Chemistryen_US
bordeaux.page4640-60en_US
bordeaux.volume57en_US
bordeaux.hal.laboratoriesMFP (Laboratoire Microbiologie Fondamentale et Pathogénicité) - UMR 5234en_US
bordeaux.issue11en_US
bordeaux.institutionCNRSen_US
bordeaux.peerReviewedouien_US
bordeaux.inpressnonen_US
bordeaux.import.sourcepubmed
hal.popularnonen_US
hal.audienceInternationaleen_US
hal.exportfalse
workflow.import.sourcepubmed
dc.rights.ccPas de Licence CCen_US
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Journal%20of%20Medicinal%20Chemistry&rft.date=2014-06-12&rft.volume=57&rft.issue=11&rft.spage=4640-60&rft.epage=4640-60&rft.eissn=1520-4804&rft.issn=1520-4804&rft.au=SUCHAUD,%20Virginie&BAILLY,%20Fabrice&LION,%20Cedric&CALMELS,%20Christina&ANDR%C3%89OLA,%20Marie-Line&rft.genre=article


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