Naamines and Naamidines as Novel Agents against a Plant Virus and Phytopathogenic Fungi.

Naamines and Naamidines as Novel Agents against a Plant Virus and Phytopathogenic Fungi.
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纳胺和纳脒作为抗植物病毒和植物病原真菌的新型药剂

DOI:
10.3390/md16090311
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发表时间:
2018-09-03
期刊:
影响因子:
5.4
通讯作者:
Wang Q
Wang Q
中科院分区:
医学2区
文献类型:
--
作者:
Guo P;Li G;Liu Y;Lu A;Wang Z;Wang Q

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合成了Naamines、Naamidines及其衍生物,并通过核磁共振(NMR)和质谱进行了表征。首次评价了这些生物碱对植物病毒和植物病原真菌的活性。苄氧基萘胺衍生物15 d在500 μg/mL浓度下对烟草花叶病毒具有较好的抑制活性(灭活活性46%,治疗活性49%,保护活性41%);其活性高于商品植物杀病毒剂利巴韦林的相应活性(分别为32%,35%和34%),使其成为抗病毒研究的有希望的新先导化合物。体外抗真菌活性测定结果表明,化合物对14种植物病原真菌具有很好的抑制作用。苄氧基萘胺衍生物15 d具有广谱的杀菌活性,有望成为杀菌研究的新先导化合物。另外的体内测定表明,许多化合物显示> 30%的抑制作用。
Naamines, naamidines and various derivatives of these marine natural products were synthesized and characterized by means of nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry. The activities of these alkaloids against a plant virus and phytopathogenic fungi were evaluated for the first time. A benzyloxy naamine derivative 15d displayed excellent in vivo activity against tobacco mosaic virus at 500 μg/mL (inactivation activity, 46%; curative activity, 49%; and protective activity, 41%); its activities were higher than the corresponding activities of the commercial plant virucide ribavirin (32%, 35%, and 34%, respectively), making it a promising new lead compound for antiviral research. In vitro assays revealed that the test compounds exhibited very good antifungal activity against 14 kinds of phytopathogenic fungi. Again, the benzyloxy naamine derivative 15d exhibited broad-spectrum fungicidal activity, emerging as a new lead compound for fungicidal research. Additional in vivo assays indicated that many of the compounds displayed inhibitory effects >30%.
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