新型抗真菌剂曲古抑菌素衍生物的合成与生物学评价
Synthesis and biological evaluation of novel trichodermin derivatives as antifungal agents.
作者信息
Zheng Min, Yao Ting-Ting, Xu Xiao-Jun, Cheng Jing-Li, Zhao Jin-Hao, Zhu Guo-Nian
机构信息
College of Agriculture and Biotechnology, Zhejiang University, Hangzhou 310029, China.
College of Agriculture and Biotechnology, Zhejiang University, Hangzhou 310029, China.
出版信息
Bioorg Med Chem Lett. 2014 Aug 1;24(15):3565-8. doi: 10.1016/j.bmcl.2014.05.047. Epub 2014 May 23.
To discover more potential antifungal agents, 17 novel trichodermin derivatives were designed and synthesized by modification of 3 and 4a. The structures of all the synthesized compounds were confirmed by (1)H NMR, ESI-MS and HRMS. Their antifungal activities against Ustilaginoidea oryzae and Pyricularia oryzae were evaluated. Most of the target compounds showed potent inhibitory activity, in which 4g showed superior inhibitory effects than 4a and commercial fungicide prochloraz. Furthermore, 4h demonstrated comparable inhibitory activity to 4a. Moreover, 4i and 4l exhibited excellent inhibitory activity for Pyricularia oryzae. Additionally, compound 9 was found to be more active against all tested fungal strains than 3, with EC50 values of 0.47 and 3.71 mg L(-1), respectively.
为发现更多潜在的抗真菌剂，通过对3和4a进行修饰设计并合成了17种新型木霉菌素衍生物。所有合成化合物的结构均通过¹H NMR、ESI-MS和HRMS得到确证。评估了它们对稻曲病菌和稻瘟病菌的抗真菌活性。大多数目标化合物表现出较强的抑制活性，其中4g的抑制效果优于4a和市售杀菌剂咪鲜胺。此外，4h表现出与4a相当的抑制活性。而且，4i和4l对稻瘟病菌表现出优异的抑制活性。此外，发现化合物9对所有测试真菌菌株的活性均高于3，其EC50值分别为0.47和3.71 mg L⁻¹。
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