College of Science, Huazhong Agricultural University, Wuhan 430070, China.
College of Science, Huazhong Agricultural University, Wuhan 430070, China.
Bioorg Med Chem Lett. 2020 Jan 15;30(2):126826. doi: 10.1016/j.bmcl.2019.126826. Epub 2019 Dec 3.
A series of γ-lactam analogs containing 1,3-benzodioxole moiety were designed, and these derivatives were synthesized from the lead compound of lactam via a structural diversity-oriented synthesis, their structures were confirmed by HNMR,CNMR, ESI-MS spectrum. Their antifungal activities were evaluated against four serious and typically crop-threatening agricultural fungi, including Rhizoctonia solani, Alternaria tenuis Nees, Gloeosporium theae-sinensis, and Fusarium graminearum. Some of these derivatives exhibited activity against Alternaria tenuis Nees higher than that of commercial fungicides carbendazim, such as compounds 7a, 7b, and 7i, compared with the blank control, some of these derivatives showed good antifungal activities against Gloeosporium theae-sinensis and Fusarium graminearum. The systematic study provides evidences for further structural modification and application of lactam analogues as antifungal agents for agriculture.
设计了一系列含有 1,3-苯并二恶茂部分的γ-内酰胺类似物，这些衍生物是通过结构多样性导向合成从内酰胺的先导化合物合成的，其结构通过 HNMR、CNMR、ESI-MS 谱得到确认。它们的抗真菌活性被评估为对四种严重且典型的作物威胁农业真菌，包括立枯丝核菌、细交链孢菌、茶拟盘多毛孢和禾谷镰刀菌。这些衍生物中的一些对细交链孢菌的活性高于商业杀菌剂多菌灵，如化合物 7a、7b 和 7i，与空白对照相比，这些衍生物中的一些对茶拟盘多毛孢和禾谷镰刀菌表现出良好的抗真菌活性。系统研究为进一步的结构修饰和应用内酰胺类似物作为农业抗真菌剂提供了证据。
