具有杀菌活性的 1-1,2,3-三唑键合的齐墩果烷型三萜类化合物。
Oleanane-Type Triterpene Conjugates with 1-1,2,3-Triazole Possessing of Fungicidal Activity.
机构信息
Key Laboratory for Northern Urban Agriculture of Ministry of Agriculture and Rural Affairs, Beijing University of Agriculture, Beijing 102206, China.
Torch High Technology Industry Development Center, Ministry of Science &Technology, Beijing 100045, China.
出版信息
Molecules. 2022 Aug 2;27(15):4928. doi: 10.3390/molecules27154928.
The triazole pesticide is an organic nitrogen-containing heterocyclic compound with a 1,2,3-Triazole ring. In order to develop a potential glucosamine-6-phosphate synthase (GlmS) inhibitor bactericide, 18 triazole-derivative compounds were synthesized efficiently. In addition, these compounds have not been reported in the literature. The structure was confirmed by high-resolution mass spectrometry (HRMS), 1H NMR and 13C NMR. The potential use of the most promising derivatives has been investigated by testing their antifungal activity and enzyme inhibitory activity, revealing inhibitory activities in the low micromolar range. Among them, the antifungal effects of compounds , , , , , and on were particularly significant, all of which were above 83%. These compounds will be further investigated as potential antifungal lead compounds. Their structure-activity relationships are discussed based on the effects of substituted phenyl groups on compounds.
三唑类农药是一种含有 1,2,3-三唑环的有机含氮杂环化合物。为了开发一种有潜力的葡萄糖胺-6-磷酸合酶（GlmS）抑制剂杀菌剂，高效合成了 18 种三唑类衍生物化合物。此外，这些化合物在文献中尚未有报道。通过高分辨率质谱（HRMS）、1H NMR 和 13C NMR 对其结构进行了确认。通过测试它们的抗真菌活性和酶抑制活性，研究了最有前途的衍生物的潜在用途，发现其具有低微摩尔范围内的抑制活性。其中，化合物 、 、 、 、 和 对 的抗真菌效果尤为显著，均高于 83%。这些化合物将作为潜在的抗真菌先导化合物进一步研究。根据取代苯基对化合物的影响，讨论了它们的构效关系。
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