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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Design, synthesis and discovery of andrographolide derivatives against Zika virus infection
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Design, synthesis and discovery of andrographolide derivatives against Zika virus infection

机译：Zika病毒感染的Andrographolide衍生物的设计，合成和发现

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The Zika endemic established by imported and local transmission is of significant concern and effective anti-ZIKV drugs remain an urgent unmet need. As andrographolide was identified to be an inhibitor of DENV and CHIKV and the importance of quinoline structure against infectious diseases was considered, we are interested in studying its andrographolide derivatives with quinoline moiety against Zika virus infection. In addition to screening eight in-house derivatives of andrographolide, sixteen new derivatives were designed, synthesized and tested against Zika virus infection. Among these compounds, two most potent anti-Zika compounds of 19-acetylated 14 alpha,-(5',7'-dichloro-8'-quinolyloxy) derivative 17b and 14 beta-(8'-quinolyloxy)-3,19- diol derivative 3 with the highest selectivity were discovered. The SAR analysis indicates that rational and optimal combined modification/s at 3-, 14-, or 19-positions can make derivatives less toxic and more potent against Zika infection, and both of 3 and 17b are suitable as leads for designing new generation of andrographolide derivatives with quinoline or its structure- and property related moieties against Zika virus and other arboviruses. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：由进口和地方传播建立的Zika流行具有重要关注，有效的抗ZIKV药物仍然是一个紧迫的未满足需求。由于andrographolide被鉴定为DENV和CHIKV的抑制剂，并且考虑了喹啉结构对传染病的重要性，我们有兴趣研究其与喹啉部分的Andropholide衍生物对Zika病毒感染。除了筛选Andrographolide的八个内部衍生物外，设计，合成并测试了Zika病毒感染的16个新衍生物。在这些化合物中，两个最有效的19-乙酰化14α， - （5'，7'-二氯-8'-喹啉氧基）衍生物17b和14β-（8'-喹啉氧基）-3,19-中的抗zika化合物 - （5'，7'-二氯-8'-喹啉）-3,19-发现了具有最高选择性的二醇衍生物3。 SAR分析表明，在3-，14-或19位的合理和最佳的组合改性/ s可以使衍生物对Zika感染的毒性和更有效，以及3和17b都适合设计新一代的引线Andrographolide衍生物与喹啉或其结构和财产相关部分对抗Zika病毒和其他枝芽孢杆菌。 （c）2019年Elsevier Masson SAS。版权所有。

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