PDF(Pubmed)
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.
摘要：
植物病原真菌对全球粮食安全构成重大威胁,生态系统服务,和人类生计。需要有效和广谱的杀真菌剂来对抗这些病原体。在这项研究中,设计并合成了一种新型的抗真菌2-氧乙酸酰肼喹喔啉支架作为简单的类似物。对灰葡萄孢菌（B.cinerea),solani（A.solani)，赤霉素(G.zeae),根瘤菌(R.solani)，弓形虫(C.orbiculare)，和链格孢菌(A.alternata)。这些结果表明，大多数化合物表现出显着的抑制活性，并且具有比吡啶细菌更好的功效。例如化合物15(针对G.zeae的EC50=0.87μg/mL，针对C.orbiculare的EC50=1.01μg/mL）和化合物1（针对A.alternata的EC50=1.54μg/mL，EC50=0.20μg/mL，对R.solani)。喹喔啉-2-氧乙酸酰肼衍生物的3D-QSAR分析为基于喹喔啉的新型抗真菌药物分子的设计和优化提供了新的见解。
