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dc.rights.licenseopenen_US
dc.contributor.authorBILLAMBOZ, Muriel
dc.contributor.authorSUCHAUD, Virginie
dc.contributor.authorBAILLY, Fabrice
dc.contributor.authorLION, Cedric
dc.contributor.authorDEMEULEMEESTER, Jonas
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.accessioned2024-03-11T15:45:28Z
dc.date.available2024-03-11T15:45:28Z
dc.date.issued2013-07-11
dc.identifier.issn1948-5875en_US
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/188691
dc.description.abstractEnA series of 2-hydroxy-1,3-dioxoisoquinoline-4-carboxamides featuring an N-hydroxyimide chelating functionality was evaluated for their inhibitory properties against human immunodeficiency virus type 1 integrase (HIV-1 IN). Several derivatives displayed low nanomolar IC50 values comparable to that of the clinically used raltegravir. A marked effect of one compound on both primary IN-catalyzed reactions, strand transfer (ST), and 3' processing (3'-P), emphasizes a novel IN inhibition mechanism establishing it as a potential new generation IN inhibitor. Substitution of the 2-hydroxyisoquinoline-1,3-dione scaffold at position 4 by carboxamido chains was beneficial for antiviral activity since reproducible low micromolar anti-HIV activities were obtained for the first time within this scaffold.
dc.language.isoENen_US
dc.subject.en2-hydroxy-1
dc.subject.en3-dioxoisoquinoline-4-carboxamide; 3′ processing; HIV; antiretroviral; integrase
dc.title.en4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors.
dc.title.alternativeACS Med Chem Letten_US
dc.typeArticle de revueen_US
dc.identifier.doi10.1021/ml400009ten_US
dc.subject.halSciences du Vivant [q-bio]/Microbiologie et Parasitologieen_US
dc.identifier.pubmed24900718en_US
bordeaux.journalACS Medicinal Chemistry Lettersen_US
bordeaux.page606-11en_US
bordeaux.volume4en_US
bordeaux.hal.laboratoriesMFP (Laboratoire Microbiologie Fondamentale et Pathogénicité) - UMR 5234en_US
bordeaux.issue7en_US
bordeaux.institutionCNRSen_US
bordeaux.peerReviewedouien_US
bordeaux.inpressnonen_US
bordeaux.import.sourcepubmed
hal.identifierhal-04454591
hal.version1
hal.date.transferred2024-03-11T15:45:31Z
hal.popularnonen_US
hal.audienceInternationaleen_US
hal.exporttrue
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=ACS%20Medicinal%20Chemistry%20Letters&rft.date=2013-07-11&rft.volume=4&rft.issue=7&rft.spage=606-11&rft.epage=606-11&rft.eissn=1948-5875&rft.issn=1948-5875&rft.au=BILLAMBOZ,%20Muriel&SUCHAUD,%20Virginie&BAILLY,%20Fabrice&LION,%20Cedric&DEMEULEMEESTER,%20Jonas&rft.genre=article


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