Institute of Chemical Engineering, Ural Federal University Named after the First President of Russia B.N. Yeltsin, 19 Mira Street, 620002 Ekaterinburg, Russia.
Postovsky Institute of Organic Synthesis, Ural Branch of Russian Academy of Sciences, 22/20 S. Kovalevskaya Street, 620108 Ekaterinburg, Russia.
Molecules. 2023 Jan 3;28(1):419. doi: 10.3390/molecules28010419.
The addition of active groups of known fungicides, or systemic acquired resistance inducers, into novel compound molecules to search for potential antifungal compounds is a popular and effective strategy. In this work, a new series of -acyl--arylalanines was developed and synthesized, in which 1,2,3-thiadiazol-5-ylcarbonyl or 3,4-dichloroisothiazol-5-ylcarbonyl (fragments from synthetic plant resistance activators tiadinil and isotianil, respectively) and a fragment of -arylalanine, the toxophoric group of acylalanine fungicides. Several new synthesized compounds have shown moderate antifungal activity against fungi in vitro, such as , and . In vivo tests against showed that compound was 92% effective at a concentration of 200 µg/mL, similar to level of tiadinil, a known inducer of systemic resistance. Thus, could be considered a new candidate fungicide for further detailed study. The present results will advance research and influence the search for more promising fungicides for disease control in agriculture.
将已知杀菌剂的活性基团或系统获得性抗性诱导剂添加到新的化合物分子中，以寻找潜在的抗真菌化合物，是一种流行且有效的策略。在这项工作中，开发并合成了一系列新的 -酰基-芳基丙氨酸，其中 1,2,3-噻二唑-5-羰基或 3,4-二氯异噻唑-5-羰基（分别来自合成植物抗性激活剂噻二唑和异噻二唑的片段）和 -芳基丙氨酸片段，是酰基丙氨酸类杀菌剂的毒性基团。一些新合成的化合物显示出对体外真菌的中等抗真菌活性，如 、 和 。对 的体内试验表明，化合物 在 200µg/mL 浓度下的有效率为 92%，与已知的系统抗性诱导剂噻二唑相当。因此， 可以被认为是进一步详细研究的一种新的候选杀菌剂。本研究结果将推进相关研究，并有助于寻找更有前景的农业病害防治用杀菌剂。
