92428-42-7Relevant articles and documents
Synthesis and Anti-Influenza Virus Effects of Novel Substituted Polycyclic Pyridone Derivatives Modified from Baloxavir
Chen, Dawei,Gao, Zhenxiong,Hou, Jinqiang,Jiang, Yuyang,Tang, Lin,Wu, Weibin,Yan, Haiyan,Zhang, Cunlong
supporting information, p. 14465 - 14476 (2021/10/12)
In this work, a series of novel substituted polycyclic pyridone derivatives were designed and synthesized as potent anti-influenza agents. The cytopathic effect (CPE) assay and cytotoxicity assay indicated that all of the compounds possessed potent anti-influenza virus activity and relatively low cytotoxicity; some of them inhibited the replication of influenza A virus (IAV) at picomolar concentrations. Further studies revealed that, at a concentration of 3 nM, three compounds (10a, 10d, and 10g) could significantly reduce the M2 RNA amounts and M2 protein expression of IAV and inhibit the activity of RNA-dependent RNA polymerase (RdRp). Among them, (R)-12-(5H-dibenzo[a,d][7]annulen-5-yl)-7-hydroxy-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione (10a) was found to be a promising anti-influenza drug candidate with good human liver microsomal stability, as well as with better selectivity index and oral bioavailability than Baloxavir.
A facile and efficient method for the synthesis of N-substituted 3-oxoisoindoline-1-carbonitrile derivatives catalyzed by sulfamic acid
Hu, Ling-Jun,Zhan, Zha-Jun,Lei, Min,Hu, Li-Hong
, p. 189 - 198 (2013/06/27)
A new and efficient method for the synthesis of N-substituted 3-oxoisoindoline-1-carbonitrile derivatives by a one-pot, three-component condensation reaction of 2-carboxybenzaldehyde, primary amine, and TMSCN in the presence of 10 mol % sulfamic acid (NH2SO3H) as the catalyst in EtOH under reflux temperature is described. The process is simple and environmentally benign and the catalyst is commercially available and inexpensive. ARKAT-USA, Inc.
Asymmetric protonation of ketone enolates using chiral β- hydroxyethers: Acidity-tuned enantioselectivity
Kim, B. Moon,Kim, Hyunwoo,Kim, Woosung,Im, Keun Young,Park, Jin Kyoon
, p. 5104 - 5107 (2007/10/03)
New chiral hydroxyethers 1a-f were prepared for asymmetric protonation of achiral enolates prepared from prochiral ketones. The enantioselectivity of protonation was highly dependent upon the acidity of the chiral alcohols, the highest enantioselectivity