法维皮拉维
核苷
前药
病毒
酶
病毒学
核苷类似物
甲型流感病毒
化学
生物
医学
立体化学
生物化学
2019年冠状病毒病(COVID-19)
传染病(医学专业)
病理
疾病
作者
Mingming Han,Xu Zhao,Xuedong Wu,Wei Huang,Xingzhou Li,Fang Yu
出处
期刊:Medicinal Chemistry
[Bentham Science Publishers]
日期:2018-01-15
卷期号:14 (6): 595-603
被引量:8
标识
DOI:10.2174/1573406414666180112102225
摘要
T-705 (Favipiravir) is a broad spectrum antiviral agent approved for stockpiling in Japan and currently in Phase 3 testing in the United States. Against influenza, it acts as a prodrug, converted intracellularly to selectively inhibit viral RNA-dependent RNA polymerase or similar enzymes. This is regarded as a novel antiviral mechanism of action, reducing crossresistance to other existing anti-influenza drugs.To develop new analogs, a class of 1,3-oxathiolane nucleoside derivatives of T-705 was designed and synthesized in this work.Anti-influenza activity and Anti-HIV activity of these compounds were evaluated. Compound 1a displayed activity against A H1N1 with an IC50 of 40.4 µmol/L. Compound 1b showed weak activity against HIV with a viral suppression rate of 70-80% at 30 µmol/L.A class of 1,3-oxathiolane nucleoside derivatives of T-705 was designed and synthesized, and one of them was identified as a novel scaffold against viral infection.
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