Synthesis and Antiviral Activity of Camphene Derivatives against Different Types of Viruses
作者:Anastasiya S. Sokolova、Valentina P. Putilova、Olga I. Yarovaya、Anastasiya V. Zybkina、Ekaterina D. Mordvinova、Anna V. Zaykovskaya、Dmitriy N. Shcherbakov、Iana R. Orshanskaya、Ekaterina O. Sinegubova、Iana L. Esaulkova、Sophia S. Borisevich、Nikolay I. Bormotov、Larisa N. Shishkina、Vladimir V. Zarubaev、Oleg V. Pyankov、Rinat A. Maksyutov、Nariman F. Salakhutdinov
DOI:10.3390/molecules26082235
日期:——
that turn out to be pathogenic for humans. Evidently, there is an urgent need for new strategies to develop efficient antiviral agents with broad-spectrum activities. In this paper, we identified camphene derivatives that showed broad antiviral activities in vitro against a panel of enveloped pathogenic viruses, including influenza virus A/PR/8/34 (H1N1), Ebola virus (EBOV), and the Hantaan virus.
迄今为止,“一种病毒一种药物”的抗病毒药物开发方法无法有效应对日益多样化的病毒所带来的持续威胁,这些病毒导致病毒感染的爆发,而这些病毒感染最终证明对人类具有致病性。显然,迫切需要新的策略来开发具有广谱活性的高效抗病毒药物。在本文中,我们鉴定了莰烯衍生物,它们在体外对一组包膜致病病毒表现出广泛的抗病毒活性,包括流感病毒 A/PR/8/34 (H1N1)、埃博拉病毒 (EBOV) 和汉坦病毒。先导化合物2a 的结构中含有吡咯烷循环,对流感病毒 (IC 50 = 45.3 µM)、埃博拉假型病毒 (IC 50 = 0.12 µM) 和真正的埃博拉病毒 (IC 50 = 18.3 µM)显示出抗病毒活性,如下所示以及针对汉坦病毒 Gn-Gc 糖蛋白的假病毒 (IC 50 = 9.1 µM)。使用假型病毒和分子模型进行的抗病毒活性研究结果表明,病毒和细胞膜之间融合过程所需的病毒表面蛋白是化合物2a的