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香豆素-3-甲酰胺衍生物的设计、合成与抗真菌活性评价。

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

机构信息

Jiangsu Key Laboratory of Pesticide, College of Sciences, Nanjing Agricultural University, Nanjing 210095, PR China.

Jiangsu Key Laboratory of Pesticide, College of Sciences, Nanjing Agricultural University, Nanjing 210095, PR China.

出版信息

Fitoterapia. 2018 Jun;127:387-395. doi: 10.1016/j.fitote.2018.03.013. Epub 2018 Apr 7.

Abstract

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, EC values of which against Rhizoctorzia solani were as low as 1.80 μg/mL, 2.50 μg/mL, 2.25 μg/mL and 2.10 μg/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.

摘要

设计并合成了一系列香豆素-3-甲酰胺/酰肼,所有目标化合物均在体外进行了抗真菌活性评估,针对灰葡萄孢、番茄早疫病菌、禾谷镰刀菌、茄链格孢、黄瓜炭疽病菌和番茄叶霉病菌进行了评估,部分设计的化合物 4a-4g 在初步测定中表现出潜在的活性,其中化合物 4a、4d、4e 和 4f 对茄链格孢的 EC 值低至 1.80μg/mL、2.50μg/mL、2.25μg/mL 和 2.10μg/mL,与阳性对照相比,对其的控制效果更好。此外,化合物 4a 和 4e 对灰葡萄孢的抗真菌活性与 Boscalid 相当。

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