56759-18-3Relevant articles and documents
Generation of potent Nrf2 activators via tuning the electrophilicity and steric hindrance of vinyl sulfones for neuroprotection
Song, Zi-Long,Hou, Yanan,Bai, Feifei,Fang, Jianguo
, (2020/12/21)
Oxidative stress is constantly involved in the etiopathogenesis of an ever-widening range of neurodegenerative diseases. As a consequence, effective repression of cellular oxidative stress to a redox homeostatic condition is a promising and feasible strategy to treat, or at least retard the progression of, such disorders. Nrf2, a primary orchestrator of cellular antioxidant response machine, is responsible for detoxifying and compensating for deleterious oxidative stress via transcriptional activation of a diverse array of antioxidant biomolecules. In the framework of our persistent interest in disclosing small molecules that interfere with cellular redox-regulating machinery, we report herein the synthesis, optimization, and biological assessment of 47 vinyl sulfone scaffold-bearing small molecules, most of which exhibit robust neuroprotective effect against H2O2-mediated lesions to PC12 cells. After initial screening, the most potent neuroprotective compounds 9b and 9c with marginal cytotoxicity were selected for the follow-up studies. Our results demonstrate that their neuroprotective effects are attributed to the up-regulation of a panel of antioxidant genes and corresponding gene products. Further mechanistic studies indicate that Nrf2 is indispensable for the cellular performances of 9b and 9c, arising from the fact that silence of Nrf2 gene drastically nullifies their protective action. Taken together, 9b and 9c discovered in this work merit further development as neuroprotective candidates for the treatment of oxidative stress-mediated pathological conditions.
Synthesis method of (E)-vinyl sulfone compound
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Paragraph 0013, (2019/01/08)
The invention discloses a synthesis method of a (E)-vinyl sulfone compound. The synthesis method comprises the following steps: using acetonitrile as a solvent, under the catalysis of SbCl3, oxidizingand reducing 1,2-alkylene oxide compound (IV) to genera
Decarboxylative sulfonylation of arylpropiolic acids with sulfinic acids: synthesis of (E)-vinyl sulfones
Meesin, Jatuporn,Katrun, Praewpan,Reutrakul, Vichai,Pohmakotr, Manat,Soorukram, Darunee,Kuhakarn, Chutima
supporting information, p. 1440 - 1446 (2017/02/15)
Decarboxylative sulfonylation of arylpropiolic acids has been achieved by simply employing Na2CO3as a promoter and arenesulfinic acids as sulfonylating reagents. This simple and environmentally benign transformation offers an alternative approach and allows for easy and rapid synthesis of E-Vinyl sulfones from arylpropiolic acids and arenesufinic acids.
