Affiliation:
1. Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing 210095, China
Abstract
Plant pathogenic fungi pose a major threat to global food security, ecosystem services, and human livelihoods. Effective and broad-spectrum fungicides are needed to combat these pathogens. In this study, a novel antifungal 2-oxyacetate hydrazide quinoxaline scaffold as a simple analogue was designed and synthesized. Their antifungal activities were evaluated against Botrytis cinerea (B. cinerea), Altemaria solani (A. solani), Gibberella zeae (G. zeae), Rhizoctonia solani (R. solani), Colletotrichum orbiculare (C. orbiculare), and Alternaria alternata (A. alternata). These results demonstrated that most compounds exhibited remarkable inhibitory activities and possessed better efficacy than ridylbacterin, such as compound 15 (EC50 = 0.87 μg/mL against G. zeae, EC50 = 1.01 μg/mL against C. orbiculare) and compound 1 (EC50 = 1.54 μg/mL against A. alternata, EC50 = 0.20 μg/mL against R. solani). The 3D-QSAR analysis of quinoxaline-2-oxyacetate hydrazide derivatives has provided new insights into the design and optimization of novel antifungal drug molecules based on quinoxaline.
Funder
National Key Research and Development Program of China
Reference38 articles.
1. Li, L., Zhu, X.-M., Zhang, Y.-R., Cai, Y.-Y., Wang, J.-Y., Liu, M.-Y., Wang, J.-Y., Bao, J.-D., and Lin, F.-C. (2022). Research on the Molecular Interaction Mechanism between Plants and Pathogenic Fungi. Int. J. Mol. Sci., 23.
2. Trends and perspectives on general Pesticide analytical chemistry;Wu;Adv. Agrochem.,2022
3. Plant Disease: A Threat to Global Food Security;Strange;Annu. Rev. Phytopathol.,2005
4. Novel 1,3,5-thiadiazine-2-thione derivatives containing a hydrazide moiety: Design, synthesis and bioactive evaluation against phytopathogenic fungi in vitro and in vivo;Wang;Chin. Chem. Lett.,2019
5. Secondary Compounds as Protective Agents;Swain;Annu. Rev. Plant Biol.,1977