Chen Ke, Deng Difan, Yin Yupeng, Xi Dongmei, Park Phumbum, Gao Wei, Liu Rui, Lei Kang
Department of Biotechnology, The University of Suwon, Hwaseong 18323, Gyeonggi-do, Republic of Korea.
College of Life Sciences, Linyi University, Linyi 276005, China.
Microorganisms. 2025 Jul 5;13(7):1588. doi: 10.3390/microorganisms13071588.
To identify fungicide lead compounds with novel scaffold and high efficacy, a library of 4,5-dihydrotetrazolo [1,5-a]thieno [2,3-e]pyridine derivatives, consisting of 10 newly synthesized compounds and 12 previously reported compounds, was evaluated for their potential as fungicide agents. In vitro bioassay results indicated that some target compounds exhibited certain antifungal activity against the tested fungi at a concentration of 50 μg/mL. Especially, compounds , , , and demonstrated promising antifungal activity against , , and , with EC values ranging from 4.61 to 6.66 μg/mL. Additionally, transcriptome analysis revealed that the molecular mode of action of compound involves the inhibition of nitrogen metabolism and the proteasome pathway. The present work demonstrates that 4,5,6,7-tetrahydrothieno [3,2-b] pyridine represents a promising lead scaffold and provides important theoretical foundations and innovative perspectives for the development of novel and highly efficient fungicides.
为了鉴定具有新型骨架和高效性的杀菌剂先导化合物，对一个由10个新合成化合物和12个先前报道的化合物组成的4,5-二氢四唑并[1,5-a]噻吩并[2,3-e]吡啶衍生物库进行了杀菌剂潜力评估。体外生物测定结果表明，一些目标化合物在50μg/mL浓度下对测试真菌表现出一定的抗真菌活性。特别是，化合物 、 、 和 对 、 和 表现出有前景的抗真菌活性，其EC值范围为4.61至6.66μg/mL。此外，转录组分析表明化合物 的分子作用模式涉及抑制氮代谢和蛋白酶体途径。目前的工作表明4,5,6,7-四氢噻吩并[3,2-b]吡啶是一个有前景的先导骨架，并为新型高效杀菌剂的开发提供了重要的理论基础和创新视角。
