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基于菲的娃儿藤碱衍生物作为潜在抗病毒药物的设计、合成及抗病毒评价

Design, synthesis, and antiviral evaluation of phenanthrene-based tylophorine derivatives as potential antiviral agents.

作者信息

Wang Kailiang, Hu Yanna, Liu Yuxiu, Mi Na, Fan Zhijin, Liu Yu, Wang Qingmin

机构信息

State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, People's Republic of China.

出版信息

J Agric Food Chem. 2010 Dec 8;58(23):12337-42. doi: 10.1021/jf103440s. Epub 2010 Nov 8.

DOI:10.1021/jf103440s
PMID:21058739
Abstract

A series of C9-substituted phenanthrene-based tylophorine derivatives (PBTs) were designed, synthesized, and first evaluated for their antiviral activities against tobacco mosaic virus (TMV). These compounds contain a phenanthrene core structure and can be synthesized some efficiently with excellent yields compared with tylophorine alkaloid. The bioassay results show that some of these compounds exhibited higher antiviral activity against TMV in vivo than tylophorine and commercial Ningnanmycin. Especially, compounds 3, 4, 9, 13, and 16 emerged as potential inhibitors of plant virus. These new findings demonstrate that these phenanthrene-based tylophorine derivatives (PBTs) represent another new template for antiviral studies and could be considered for novel therapy against plant virus infection.

摘要

设计、合成了一系列C9取代的菲基娃儿藤碱衍生物(PBTs),并首次评估了它们对烟草花叶病毒(TMV)的抗病毒活性。这些化合物含有菲核心结构,与娃儿藤碱生物碱相比,能够以优异的产率高效合成。生物测定结果表明,其中一些化合物在体内对TMV的抗病毒活性高于娃儿藤碱和市售的宁南霉素。特别是,化合物3、4、9、13和16成为植物病毒的潜在抑制剂。这些新发现表明,这些菲基娃儿藤碱衍生物(PBTs)代表了抗病毒研究中的另一种新模板,可考虑用于针对植物病毒感染的新疗法。

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