Chemical Engineering College, Xinjiang Agricultural University, Urumqi 830052, China.
Department of Physiology, Preclinical School, Xinjiang Medical University, Urumqi 830011, China.
Molecules. 2018 Nov 16;23(11):3002. doi: 10.3390/molecules23113002.
Umbelliferone was discovered to be an important allelochemical in our previous study, but the contribution of its activity and structure has not yet been revealed. In this study, a series of analogues were synthesized to determine the skeleton of umbelliferone and examine its fungicidal activity. Furthermore, targeted modifications were conducted with three plant parasitic fungi to examine the lead compounds. Among those tested, compounds and were found to show excellent antifungal activity with an inhibitory rate over 80% at 100 ug/mL. The study proves that umbelliferone can be a promising skeleton for fungicides discovery. In addition, the primary structure⁻activity relationship provides a good guidance for the discovery of novel fungicides based on natural products in the future.
在我们之前的研究中，发现伞形酮是一种重要的化感物质，但它的活性和结构的贡献尚未被揭示。在这项研究中，合成了一系列类似物，以确定伞形酮的骨架并检查其杀菌活性。此外，还对三种植物寄生真菌进行了靶向修饰，以检查先导化合物。在测试的化合物中，化合物 和 表现出优异的杀菌活性，在 100μg/mL 时抑制率超过 80%。该研究证明伞形酮可以成为杀菌剂发现的有前途的骨架。此外，构效关系为基于天然产物的新型杀菌剂的发现提供了良好的指导。
