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dc.creatorBazan, Hernan A.
dc.creatorBhattacharjee, Surjyadipta
dc.creatorBurgos, Carolina
dc.creatorRecio, Javier
dc.creatorAbet, Valentina
dc.creatorPahng, Amanda R.
dc.creatorJun, Bokkyoo
dc.creatorHeap, Jessica
dc.creatorLedet, Alexander J.
dc.creatorGordon, William C.
dc.creatorEdwards, Scott
dc.creatorPaul, Dennis
dc.creatorAlvarez-Builla, Julio
dc.creatorBazan, Nicolas G.
dc.date.accessioned2020-09-10T16:25:46Z
dc.date.available2020-09-10T16:25:46Z
dc.date.created2020-06-30
dc.identifier.issn0223-5234spa
dc.identifier.otherhttps://www.sciencedirect.com/science/article/pii/S0223523420305729?via%3Dihubspa
dc.identifier.urihttp://hdl.handle.net/20.500.12010/13109
dc.format.extent19 páginasspa
dc.format.mimetypeapplication/pdfspa
dc.language.isoengspa
dc.publisherEuropean Journal of Medicinal Chemistryspa
dc.sourcereponame:Expeditio Repositorio Institucional UJTLspa
dc.sourceinstname:Universidad de Bogotá Jorge Tadeo Lozanospa
dc.subjectNovel acetaminophen/paracetamol analogsspa
dc.subjectHepatotoxicityspa
dc.subjectAnalgesiaspa
dc.subjectAntipyresisspa
dc.subjectAPAP-induced liver injury (AILI)spa
dc.subjectDrug-drug interaction (DDI)spa
dc.titleA novel pipeline of 2-(benzenesulfonamide)-N-(4-hydroxyphenyl) acetamide analgesics that lack hepatotoxicity and retain antipyresisspa
dc.type.localArtículospa
dc.subject.lembSíndrome respiratorio agudo gravespa
dc.subject.lembCOVID-19spa
dc.subject.lembSARS-CoV-2spa
dc.subject.lembCoronavirusspa
dc.rights.accessrightsinfo:eu-repo/semantics/restrictedAccessspa
dc.type.hasversioninfo:eu-repo/semantics/acceptedVersionspa
dc.rights.localAcceso restringidospa
dc.identifier.doihttps://doi.org/10.1016/j.ejmech.2020.112600spa
dc.description.abstractenglishAlthough acetaminophen (ApAP) is one of the most commonly used medicines worldwide, hepatotoxicity is a risk with overdose or in patients with compromised liver function. ApAP overdose is the most common cause of acute fulminant hepatic failure. Oxidation of ApAP to N-acetyl-p-benzoquinone imine (NAPQI) is the mechanism for hepatotoxicity. 1 is a non-hepatotoxic, metabolically unstable lipophilic ApAP analog that is not antipyretic. The newly synthesized 3 is a non-hepatotoxic ApAP analog that is stable, lipophilic, and retains analgesia and antipyresis. Intraperitoneal or po administration of the new chemical entities (NCEs), 3b and 3r, in concentrations equal to a toxic dose of ApAP did not result in the formation of NAPQI. Unlike livers from NCE-treated mice, the livers from ApAP-treated mice demonstrated large amounts of nitrotyrosine, a marker of mitochondrial free radical formation, and loss of hepatic tight junction integrity. Given the widespread use of ApAP, hepatotoxicity risk with overuse, and the ongoing opioid epidemic, these NCEs represent a novel, non-narcotic therapeutic pipeline.spa
dc.type.coarhttp://purl.org/coar/resource_type/c_6501spa


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