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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Antibacterial to antifungal conversion of neamine aminoglycosides through alkyl modification. Strategy for reviving old drugs into agrofungicides.
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Antibacterial to antifungal conversion of neamine aminoglycosides through alkyl modification. Strategy for reviving old drugs into agrofungicides.

机译：通过烷基修饰将氨基胺糖苷进行抗菌到抗真菌的转化。将旧药复兴为杀真菌剂的策略。

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摘要

Many Actinomycetes aminoglycosides are widely used antibiotics. Although mainly antibacterials, a few known aminoglycosides also inhibit yeasts, protozoans and important crop pathogenic fungal oomycetes. Here we show that attachment of a C8 alkyl chain to ring III of a neamine-based aminoglycoside specifically at the 4''-o position yields a broad-spectrum fungicide (FG08) without the antibacterial properties typical for aminoglycosides. Leaf infection assays and greenhouse studies show that FG08 is capable of suppressing wheat fungal infections by Fusarium graminearum-the causative agent of Fusarium head blight-at concentrations that are minimally phytotoxic. Unlike typical aminoglycoside action of ribosomal protein translation miscoding, FG08's antifungal action involves perturbation of the plasma membrane. This antibacterial to antifungal transformation could pave the way for the development of a new class of aminoglycoside-based fungicides suitable for use in crop disease applications. In addition, this strategy is an example of reviving a clinically obsolete drug by simple chemical modification to yield a new application.
机译：许多放线菌氨基糖苷是广泛使用的抗生素。尽管主要是抗菌剂，但一些已知的氨基糖苷类也能抑制酵母菌，原生动物和重要的农作物病原性真菌卵菌。在这里，我们显示C8烷基链连接到基于神经胺的氨基糖苷的III环上，特别是在4''-o位置会产生广谱杀菌剂（FG08），而没有典型的氨基糖苷类抗菌特性。叶片感染试验和温室研究表明，FG08能够抑制枯萎病致病因子禾谷镰孢（Fusarium graminearum）的小麦真菌感染，其浓度低至对植物无害。与核糖体蛋白翻译错误编码的典型氨基糖苷作用不同，FG08的抗真菌作用涉及质膜的扰动。这种从抗菌剂到抗真菌剂的转化可为开发适用于农作物疾病应用的新型氨基糖苷类杀菌剂铺平道路。另外，该策略是通过简单的化学修饰来复活临床过时药物以产生新应用的示例。

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