36953-37-4Relevant articles and documents
NOVEL COMPOUNDS AS NADPH OXIDASE INHIBITORS
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Paragraph 0285; 0286, (2020/04/09)
The present invention is related to new compounds, pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
Concise Entries to 4-Halo-2-pyridones and 3-Bromo-4-halo-2-pyridones
Honraedt, Aurélien,Gallagher, Timothy
, p. 67 - 69 (2015/12/26)
Methods for the synthesis of both simple 4-halo-2-pyridones and more functionalized 3,4-di- and (3,4,5-tri)-halo-2-pyridones are described that are based on a combination of Sandmeyer and regioselective (copper-mediated) halogenation, with a 2-chloro or a 2-benzyloxy moiety serving as a masked 2-pyridone.
Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: Role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats
Litchfield, John,Sharma, Raman,Atkinson, Karen,Filipski, Kevin J.,Wright, Stephen W.,Pfefferkorn, Jeffrey A.,Tan, Beijing,Kosa, Rachel E.,Stevens, Benjamin,Tu, Meihua,Kalgutkar, Amit S.
scheme or table, p. 6262 - 6267 (2010/11/18)
Previous studies on the in vitro metabolism of 4-alkylsulfonyl-2-pyridone- based glucokinase activators revealed a facile, non-enzymatic displacement of the 4-alkylsulfonyl group by glutathione. In the present studies, a role for glutathione-S-transferases (GST) as catalysts in the desulfonylation reaction was demonstrated using a combination of human liver microsomes, human liver cytosol and human GSTs. The identification of a glutathione conjugate in circulation following intravenous administration of a candidate 4-methylsulfonyl-2-pyridone to rats confirmed the relevance of the in vitro findings.