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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >One-pot synthesis and antifungal activity against plant pathogens of quinazolinone derivatives containing an amide moiety
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One-pot synthesis and antifungal activity against plant pathogens of quinazolinone derivatives containing an amide moiety

机译:含酰胺部分的喹唑啉酮衍生物的一锅合成和对植物病原体的抗真菌活性

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An efficient one-pot, three-component synthesis of quinazolinone derivatives containing 3-acrylamino motif was carried out using CeO2 nanoparticles as catalyst. Thirty-nine synthesized compounds were obtained with satisfied yield and elucidated by spectroscopic analysis. Four phytopathogenic fungi were chosen to test the antifungal activities by minimum inhibitory concentration (MIC) method. Compounds 4ag, 4bb, 4bc showed broad antifungal activities against at least three fungi, and dramatic effects of substituents on the activities were observed. Docking studies were established to explore the potential antifungal mechanism of quinazolinone derivatives as the chitinase inhibitors, and also verified the importance of the amide moiety. (C) 2016 Elsevier Ltd. All rights reserved.
机译:以CeO2纳米粒子为催化剂,对含有3-丙烯酰胺基的喹唑啉酮衍生物进行了高效的一锅三组分合成。以满意的产率获得了三十九种合成化合物,并通过光谱分析进行了阐明。通过最小抑菌浓度(MIC)方法,选择了四种植物病原真菌来测试其抗真菌活性。化合物4ag,4bb,4bc对至少三种真菌显示出广泛的抗真菌活性,并且观察到取代基对活性的显着影响。建立了对接研究,以探索喹唑啉酮衍生物作为几丁质酶抑制剂的潜在抗真菌机制,并验证了酰胺部分的重要性。 (C)2016 Elsevier Ltd.保留所有权利。

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