Synthesis of<scp>d</scp>-(+)-camphor-based<i>N</i>-acylhydrazones and their antiviral activity
作者:Kseniya S. Kovaleva、Fedor I. Zubkov、Nikolay I. Bormotov、Roman A. Novikov、Pavel V. Dorovatovskii、Victor N. Khrustalev、Yuriy V. Gatilov、Vladimir V. Zarubaev、Olga I. Yarovaya、Larisa N. Shishkina、Nariman F. Salakhutdinov
DOI:10.1039/c8md00442k
日期:——
including 2D NMR spectroscopy, mass spectrometry, and X-ray diffraction analysis. In vitro screening for activity against vaccinia virus (VV) and influenza H1N1 virus was carried out for the obtained compounds. It was revealed that the derived N-acylhydrazones exhibited significant antiviralactivity with a selectivity index >280 against VV for the most promising compound.
介绍了一系列对牛痘和流感病毒具有抑制活性的新型D -(+)-樟脑N-酰基腙的设计和合成。已经开发了一种获得基于樟脑的N-酰基腙的简单途径,该途径在其结构中含有脂肪族、芳香族和杂环药效团支架。通过一整套光谱表征技术,包括二维核磁共振光谱、质谱和 X 射线衍射分析,对合成的腙的构象和构型进行了彻底的表征。对获得的化合物进行了针对牛痘病毒(VV)和流感H1N1病毒的体外活性筛选。结果表明,导出的N对于最有希望的化合物,-酰基腙表现出显着的抗病毒活性,对 VV 的选择性指数 > 280。