Synthesis and biological evaluation of substituted indole and its analogs as influenza A virus inhibitors
作者:Xuandi Zhang、Guo-Ning Zhang、Yujia Wang、Mei Zhu、Juxian Wang、Ziqiang Li、Donghui Li、Shan Cen、Yucheng Wang
DOI:10.1002/cbdv.201800577
日期:——
innovative inhibitors with a different mode of action are urgently needed. The lead compound 6092B‐E5 has proven to be an effective antiviral reagent in our previous work. Using the principles of substitution and bioisosterism of the indole ring, six series of novel anti‐IAV target products were designed, synthesized and evaluated for their antiviral effect in this work. Compounds D1, D3, D9, G1, G3
甲型流感病毒 (IAV) 是一种对人类具有高致病性的病毒,最容易发生突变,因此会导致迅速、严重的全球大流行,导致全球数百万人死亡。由于对现有抗流感药物的耐药性正在发展,迫切需要具有不同作用方式的创新抑制剂。在我们之前的工作中,先导化合物 6092B-E5 已被证明是一种有效的抗病毒试剂。在这项工作中,利用吲哚环的取代和生物等排原理,设计、合成了六个系列的新型抗 IAV 靶标产品并评估了它们的抗病毒作用。化合物 D1、D3、D9、G1、G3、G12 和 G23 被确定为有前景的抗 IAV 候选物,具有出色的抗 IAV 功效(IC50 值为 3.06-5.77 μm)和低细胞毒性(CC50 值高达和超过 100 μm) .