寨卡病毒
苯甲腈
病毒学
黄病毒
维罗细胞
药品
病毒
小头畸形
化学
药理学
医学
儿科
药物化学
作者
Yanni Quan,Rui Zhou,Bo Yang,Lidan Wang,Yujia Wang,Yingjie Ji,Yanping Li,Shan Cen
标识
DOI:10.1016/j.bioorg.2022.106265
摘要
Zika virus (ZIKV) infection could cause severe neurological complications such as neonatal microcephaly, Guillain-Barré syndrome, and myelitis in adults. No vaccine or therapeutic drug is available for prevention and control of ZIKV infection yet. Based on previously reported anti-ZIKV hit compound 1, a series of novel N-benzoyl or phenylsulfonyl substituted 2-(piperazin-1-yl)methyl-benzonitrile (PMBN) derivatives was designed, synthesized, and investigated for the antiviral activity against ZIKV replication in different cell-based phenotypic assays. The results indicated that N-phenylsulfonyl-PMBN derivative 24 displayed the comparable antiviral activity and higher oral availability than hit compound 1. Meanwhile, mechanism of action study confirmed that compound 24 acts on the early entry stage of ZIKV life cycle. The identification of this new ZIKV entry inhibitor chemotype provided a promising lead for further optimization to develop new drug for ZIKV infection.
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