About: A novel pipeline of 2-(benzenesulfonamide)-N-(4-hydroxyphenyl) acetamide analgesics that lack hepatotoxicity and retain antipyresis

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About: A novel pipeline of 2-(benzenesulfonamide)-N-(4-hydroxyphenyl) acetamide analgesics that lack hepatotoxicity and retain antipyresis Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	A novel pipeline of 2-(benzenesulfonamide)-N-(4-hydroxyphenyl) acetamide analgesics that lack hepatotoxicity and retain antipyresis
Creator	Edwards, S Edwards, Scott Paul, D Abet, V Abet, Valentina Alvarez-Builla, J Alvarez-Builla, Julio Bazan, H Bazan, Hernan Bazan, N Bhattacharjee, S Bhattacharjee, Surjyadipta Burgos, C Burgos, Carolina Gordon, W Gordon, William Heap, J Heap, Jessica Jun, Bokkyoo Ledet, A Ledet, Alexander Pahng, A Pahng, Amanda Paul, Dennis Recio, J Recio, Javier
Source	Elsevier; Medline; PMC
abstract	Although 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.
has issue date	2020-06-30(xsd:dateTime)
bibo:doi	10.1016/j.ejmech.2020.112600
bibo:pmid	32629335
has license	no-cc
sha1sum (hex)	8efc92d06bc6c80ef150457aa584a00bc7c88fe9
schema:url	https://doi.org/10.1016/j.ejmech.2020.112600
resource representing a document's title	A novel pipeline of 2-(benzenesulfonamide)-N-(4-hydroxyphenyl) acetamide analgesics that lack hepatotoxicity and retain antipyresis
has PubMed Central identifier	PMC7324353
has PubMed identifier	32629335
schema:publication	Eur J Med Chem
resource representing a document's body	covid:8efc92d06bc6c80ef150457aa584a00bc7c88fe9#body_text
is schema:about of	named entity 'analgesics' named entity 'LDH' named entity 'LC-MS/MS' named entity 'H&E' named entity 'antioxidant' named entity 'NaCl' named entity 'ApAP' named entity 'ApAP' named entity 'NAPQI' named entity 'mmol' named entity 'liver injury' named entity 'opioids' named entity 'opioids' named entity 'drug injection' named entity '4-aminophenol' named entity 'liver' named entity 'cytotoxicity' named entity 'acetaminophen' named entity 'ApAP' named entity 'ApAP' named entity 'hydrochloride' named entity 'molecular structure' named entity 'hepatic' named entity 'ApAP' named entity 'NAPQI' named entity 'lipophilicity' named entity 'retention time' named entity 'liver' named entity 'hepatotoxic' named entity 'alanine aminotransferase' named entity 'm/z' named entity 'hepatotoxicity' named entity 'ApAP' named entity 'alkaline phosphatase' named entity 'U.S. 21' named entity 'cytotoxicity' named entity 'hepatotoxic' named entity 'U.S.' named entity 'multiple comparisons' named entity 'Zonula Occludens' named entity 'visceral pain' named entity 'chronic pain' named entity 't-test' named entity 'p-aminophenol' named entity 'chicken wire' named entity 'GraphPad Prism' named entity 'ApAP' named entity 'mmol' named entity 'AST' named entity 'GSH' named entity 'nitrogen species' named entity 'ApAP' named entity 'ApAP' named entity 'LDH' named entity 'mmol' named entity 'LDH'

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