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基于天然肉酸支架的类仿制药:合成,生物评估和结构-活性关系

Lirong Guo¹, Hexiang Wang¹, Fang Liu²

¹Key Lab of Microbial Pesticides (Ministry of Agriculture and Rural Affairs), National Biopesticide Engineering Research Centre, Hubei Biopesticide Engineering Research Centre, Hubei Academy of Agricultural Sciences, Wuhan 430064, China; College of Chemistry, Huazhong Agricultural University, Wuhan 430070, China.

Pesticide biochemistry and physiology

|July 31, 2025

概括

合成和评估了21种基于肉酸的类药物,以检测其抗真菌活性. 化合物I-1显示出对Sclerotinia sclerotiorum的强烈抑制,破坏真菌菌根,并揭示出一种特定的结合机制.

科学领域:

农业化学农业化学
菌类学菌类学是指菌类学.
药用化学医学化学

背景情况:

植物病原菌在全球范围内造成重大作物损失.
自然产品为开发新型抗真菌剂提供了支架.
结构-活性关系 (SAR) 研究对于优化生物活性化合物至关重要.

研究的目的:

为了合成和评估基于肉酸的类药物作为潜在的抗真菌剂.
为了识别具有针对关键植物病原菌的特定抑制活性的化合物.
阐明强效抗真菌候选药物的作用机制和分子相互作用.

主要方法:

从天然产品支架 (CSDK450160) 中合成的21种类模拟剂.
在体外对12种植物病原菌进行了生物测试.
在植物抗真菌检测和扫描电子显微镜 (SEM) 中进行形态分析.
分子对接和量子化学计算来预测目标相互作用.

主要成果:

肉酸-联体表现出结构依赖的抗真菌特异性.
化合物I-1显示出对 Botrytis cinerea 和 Sclerotinia sclerotiorum 的显著抑制功效.
SEM发现I-1诱导了Sclerotinia sclerotiorum hyphae的严重形态损伤.
分子建模表明I-1通过π-π堆叠选择性结合到标蛋白.

结论:

由SAR驱动的优化产生了强大的抗真菌模仿剂.
化合物I-1是控制Sclerotinia sclerotiorum感染的有希望的候选物.
这项研究提供了对肉酸衍生物抗真菌活性分子基础的见解.

关键词:

生物活动是生物活动.锡南酸是一种酸.结合在一起的配偶.自然产品是一种自然产品.类模拟剂类模拟剂沙尔 (SARs) 是一种针对性搜索引擎.

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