Design, synthesis and antifungal activity evaluation of coumarin-3-carboxamide derivatives

被引:46
|
作者
Yu, Xiang [1 ]
Teng, Peng [1 ]
Zhang, Ya-Ling [1 ]
Xu, Zhao-Jun [1 ]
Zhang, Ming-Zhi [1 ]
Zhang, Wei-Hua [1 ]
机构
[1] Nanjing Agr Univ, Coll Sci, Jiangsu Key Lab Pesticide, Nanjing 210095, Jiangsu, Peoples R China
基金
国家重点研发计划;
关键词
Coumarin; Amide; Hydrazide; Synthesis; Antifungal activity; SAR; MICROWAVE-ASSISTED SYNTHESIS; METAL-FREE CONDITIONS; COUMARIN DERIVATIVES; BIOLOGICAL-ACTIVITY; MEDICINAL CHEMISTRY; ANALOGS; CYCLIZATION; ACIDS;
D O I
10.1016/j.fitote.2018.03.013
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of coumarin-3-carboxamides/hydrazides have been designed and synthesized, all the target compounds were evaluated in vitro for their antifungal activity against Botrytis cinerea, Alternaria solani, Gibberella zeae, Rhizoctorzia solani, Cucumber anthrax and Alternaria leaf spot, some of the designed compounds 4a-4g exhibited potential activity in the primary assays, this highlighted by the compounds 4a, 4d, 4e and 4f, EC50 values of which against Rhizoctorzia solani were as low as 1.80 mu g/mL, 2.50 mu g/mL, 2.25 mu g/mL and 2.10 mu g/mL, respectively, exhibiting more effective control with that of the positive control than Boscalid. Furthermore, compounds 4a and 4e represented equivalent antifungal activity with Boscalid against Botrytis cinerea.
引用
收藏
页码:387 / 395
页数:9
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