102653-50-9Relevant articles and documents
Discovery of pyrimidine nucleoside dual prodrugs and pyrazine nucleosides as novel anti-HCV agents
Guo, Shuang,Xu, Mingshuo,Guo, Qi,Zhu, Fuqiang,Jiang, Xiangrui,Xie, Yuanchao,Shen, Jingshan
, p. 748 - 759 (2019)
To explore the application potential of dual prodrug strategies in the development of anti-HCV agents, a variety of sofosbuvir derivatives with modifications at the C4 or N3 position of the uracil moiety were designed and synthesized. Some compounds exhibited potent anti-HCV activities, such as 4e and 8a–8c with similar EC50 values (0.20–0.22 μM) comparative to that of sofosbuvir (EC50 = 0.18 μM) in a genotype 1b based replicon Huh-7 cell line. Moreover, 8b displayed a good human plasma stability profile, and was easily metabolized in human liver microsomes expectantly. On the other hand, aiming to discover novel anti-HCV nucleosides, pyrazin-2(1H)-one nucleosides and their phosphoramidate prodrugs were investigated. Several active compounds were discovered, such as 25e (EC50 = 7.3 μM) and S-29b (EC50 = 19.5 μM). This kind of nucleosides were interesting and would open a new avenue for the development of antiviral agents.
Development of a functionalizable external β-turn mimic based on a cis-fused 1,7-naphthyridine scaffold
Rombouts, Frederik J. R.,De Borggraeve, Wim M.,Delaere, David,Froeyen, Matheus,Toppet, Suzanne M.,Compernolle, Frans,Hoornaert, Georges J.
, p. 1868 - 1878 (2007/10/03)
An intramolecular Diels-Alder strategy using 2(1H)-pyrazinones was applied to generate a substituted perhydro-1,7-naphthyridine ring system that served as a scaffold to construct the type VI β-turn mimic 2, featuring a cis-amide linkage between the centra
Studies on Pyrazines. 13. Chlorination of 1-Hydroxy-2(1H)-pyrazinones with Phosphoryl Chloride. Formation of 2,5-Dichloro-3-phenylpyrazine from 1-Hydroxy-3-phenyl-2(1H)-pyrazinone
Sato, Nobuhiro
, p. 149 - 152 (2007/10/02)
The chlorination of 1-hydroxy-3-phenyl-2(1H)-pyrazinone with phosphoryl chloride proceeded to 5-chloro-3-phenyl-2(H)-pyrazinone or 2,5-dichloro-3-phenylpyrazine on heating to elevated temperatures.To define the mechanism of the novel formation, reactions