Synthesis and antiviral activity of 1-hydroxy-2-(2-hydroxyphenyl)imidazoles against vaccinia virus
作者:P. A. Nikitina、N. I. Bormotov、L. N. Shishkina、A. Ya. Tikhonov、V. P. Perevalov
DOI:10.1007/s11172-019-2467-6
日期:2019.3
Abstract2-(2-Hydroxyplienyl)imidazole derivatives were synthesized and tested for antiviral activityagainstvacciniavirus in Vero cell culture. 1-Methylimidazole 3-oxides, 1-methoxyimidazoles, and 1H-imidazoles showed no activity, whereas some 1-hydroxyimidazole derivatives hold promise, exhibiting antiviral activity and weak cytotoxicity.
摘要 合成了 2-(2-Hydroxyplienyl) 咪唑衍生物,并在 Vero 细胞培养物中测试了其对痘苗病毒的抗病毒活性。1-甲基咪唑3-氧化物、1-甲氧基咪唑和1H-咪唑没有活性,而一些1-羟基咪唑衍生物具有抗病毒活性和弱细胞毒性。
Cyanoformamides are prevalent as versatile building blocks for accessing synthetically useful intermediates and biologically active compounds. The development of a milder, simpler, and more efficient approach to cyanoformamides is nontrivial. Herein, we demonstrate the effectiveness of 4,S-dioxo-imidazolinium cation activation for transforming 1-aryl-1-carbamoyl oximes to cyanoformamides. By making use of the readily available and highly modifiable dichloroimidazolidinediones (DCIDs), this novel method of activation offers reactivity remarkably greater than that of other reported protocols, exhibits a high functional group compatibility with mild conditions, and could be scaled up easily. More than 30 examples are demonstrated with good to excellent yields in short reaction times. This research not only provides a mild and efficient alternative approach to assembling a portfolio of cyanoformamides but also extends the dichloroimidazolidinedione-mediated chemistry to encompass the C-C bond cleavage reaction.