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发现氨基酸功能化的多重替代金素作为抗肠病毒新型有效抗病毒剂

Fuqiang Zheng^1,2, Junkun Ren¹, Wula Alateng²

¹Key Lab of Microbial Pesticides (Ministry of Agriculture and Rural Affairs), National Biopesticide Engineering Research Centre, Hubei Centre of Technology Innovation for Biopesticide, Hubei Biopesticide Engineering Research Centre, Hubei Academy of Agricultural Sciences, Wuhan 430064, China.

Journal of medicinal chemistry

|January 22, 2026

概括

具有氨基酸单元的新型皮里米丁衍生物显示出作为抗病毒药物的前景. 化合物8d针对肠道病毒71 (EV71),而8e对萨基病毒B3 (CVB3) 有效,增强宿主防御通路.

科学领域:

药用化学医学化学
病毒学病毒学
分子生物学分子生物学

背景情况:

病毒传染病对全球健康构成重大威胁,需要开发新型抗病毒疗法.
肠道病毒,如EV71和CVB3,是普遍存在的,缺乏特定的治疗方法,突出强调迫切需要新的治疗策略.
氨基酸是生物过程的基础,使它们成为药物设计的有吸引力的组件.

研究的目的:

设计和合成包含氨基酸单元的新型多替代胺衍生物.
评估这些化合物的抗病毒疗效对抗肠道病毒71 (EV71) 和Coxsackievirus B3 (CVB3).
阐明最强大的抗病毒化合物的作用机制.

主要方法:

新型多替代型胺衍生物的合成,与氨基酸部分功能化.
使用细胞病变效应抑制试验对EV71和CVB3进行抗病毒活性查.
活性化合物的EC50值的确定.
作用机制研究,包括评估病毒蛋白酶的抑制 (2Apro,3Cpro,3Dpol) 和分析宿主细胞通路 (I型干扰素信号传递).

主要成果:

化合物8d显示出显著的抗EV71活性,EC50为12.86 ± 0.61μM.
化合物8e表现出强大的抗CVB3活性,EC50为11.72±1.01μM.
这些化合物主要在EV71的感染后复制阶段起作用,并没有直接抑制关键的病毒蛋白酶;相反,它们激活了细胞I型干扰素信号通路.

结论:

氨基酸功能化的pyrimidines代表了抗病毒药物开发的一类有前途的化合物.
化合物8d和8e分别表现出针对EV71和CVB3的特定和强大的抗病毒活性.
已识别的化合物通过I型干扰素途径增强宿主抗病毒防御,这表明一种独特的治疗机制.

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