1,2,4-恶二唑类苯甲酰胺生物等排体的合成、生物活性及对斑马鱼胚胎的毒性
1,2,4-Oxadiazole-Based Bio-Isosteres of Benzamides: Synthesis, Biological Activity and Toxicity to Zebrafish Embryo.
机构信息
College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
出版信息
Int J Mol Sci. 2021 Feb 27;22(5):2367. doi: 10.3390/ijms22052367.
To discover new compounds with broad spectrum and high activity, we designed a series of novel benzamides containing 1,2,4-oxadiazole moiety by bioisosterism, and 28 benzamides derivatives with antifungal activity were synthesized. These compounds were evaluated against four fungi: , , , and . The results indicated that most of the compounds displayed good fungicidal activities, especially against . For example, (84.4%), (83.6%), (83.3%), (83.1%), (83.3%), and (83.6%) were better than pyraclostrobin (81.4%) at 100 mg/L. In addition, the acute toxicity of to zebrafish embryo was 20.58 mg/L, which was classified as a low-toxicity compound.
为了发现广谱、高效的新化合物，我们通过生物等排原理设计了一系列含 1,2,4-噁二唑片段的新型苯甲酰胺类化合物，合成了 28 个具有抗真菌活性的苯甲酰胺衍生物。这些化合物对四种真菌进行了评估：、、、和。结果表明，大多数化合物表现出良好的杀菌活性，尤其是对。例如，化合物 (84.4%)、(83.6%)、(83.3%)、(83.1%)、(83.3%)和 (83.6%)在 100mg/L 时优于吡唑醚菌酯（81.4%）。此外，化合物 对斑马鱼胚胎的急性毒性为 20.58mg/L，属于低毒性化合物。
Zotero 插件