100129-35-9Relevant articles and documents
Design, synthesis and in vitro biological evaluation of isoxazol-4-carboxa piperidyl derivatives as new anti-influenza A agents targeting virus nucleoprotein
Pei, Shuchen,Xia, Shihao,Yang, Fating,Chen, Junlin,Wang, Mengdie,Sun, Wanlin,Li, Ziqiang,Yuan, Kangyao,Chen, Jun
, p. 4446 - 4454 (2020/02/13)
Influenza infection is a major cause of morbidity and mortality during seasonal epidemics and sporadic pandemics. It is important and urgent to develop new anti-influenza agents with a new mechanism of action. Nucleozin has been reported as a potent antagonist of nucleoprotein accumulation in the nucleus. In this study, a new series of isoxazol-4-carboxa piperidyl derivatives 1a-j were synthesized and their chemical structures were confirmed by 1H, 13C NMR and mass spectral data. Furthermore, all the synthesized compounds were evaluated for in vitro anti-influenza virus activity against influenza virus (A/PR/8/34 H1N1). Among all the compounds, 1a, 1b, 1c, 1f and 1g exhibited more potent activity than the standard drug, and compound 1b has showed most promising anti-influenza virus activity. These results are also consistent with the docking study results in terms of the design of compounds targeting influenza A via viral nucleoprotein.
Superacid-catalyzed preparation of aryl-substituted piperidines via dicationic electrophiles
Klumpp, Douglas A.,Beauchamp, Philip S.,Sanchez Jr., Gregorio V.,Aguirre, Sharon,De Leon, Sarah
, p. 5821 - 5823 (2007/10/03)
The electrophilic chemistry of 1,2,3,6-tetrahydropyridines has been studied in the Bronsted superacid, CF3SO3H (triflic acid). The 1,2,3,6-tetrahydropyridines react with arenes to give aryl-substituted piperidines. It is proposed tha
