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喹啉连接 1,2,4-恶二唑取代的苯甲酰胺:合成、生物活性及对斑马鱼胚胎的毒性。

Benzamides Substituted with Quinoline-Linked 1,2,4-Oxadiazole: 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

Molecules. 2022 Jun 20;27(12):3946. doi: 10.3390/molecules27123946.

Abstract

To develop new compounds with high activity, broad spectrum and low-toxicity, 17 benzamides substituted with quinoline-linked 1,2,4-oxadiazole were designed using the splicing principle of active substructures and were synthesized. The biological activities were evaluated against 10 fungi, indicating that some of the synthetic compounds showed excellent fungicidal activities. For example, at 50 mg/L, the inhibitory activity of (3-Cl-4-Cl substituted, 86.1%) against was superior to that of quinoxyfen (77.8%), and the inhibitory activity of (3-CF substituted, 77.8%) was comparable to that of quinoxyfen. The fungicidal activities of and to were better than that of quinoxyfen (14.19 mg/L), with EC of 6.67 mg/L and 5.17 mg/L, respectively. Furthermore, the acute toxicity of was 19.42 mg/L, classifying it as a low-toxic compound.

摘要

为了开发具有高活性、广谱和低毒性的新化合物,采用活性亚结构拼接原理,设计并合成了 17 个带有喹啉连接的 1,2,4-噁二唑取代的苯甲酰胺。对 10 种真菌进行了生物活性评价,结果表明部分合成化合物表现出优异的杀菌活性。例如,在 50mg/L 时,化合物 (3-Cl-4-Cl 取代,86.1%) 对 的抑制活性优于喹氧灵 (77.8%),化合物 (3-CF 取代,77.8%) 的抑制活性与喹氧灵相当。化合物 和 对 的杀菌活性优于喹氧灵(14.19mg/L),EC 分别为 6.67mg/L 和 5.17mg/L。此外,化合物 的急性毒性为 19.42mg/L,属于低毒化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a327/9229796/95ed31d9112d/molecules-27-03946-g001.jpg

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