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基于天然产物的杀菌剂:2H-色烯衍生物的合成及对植物病原菌的抑菌活性。

Natural Products-Based Fungicides: Synthesis and Antifungal Activity against Plant Pathogens of 2H-Chromene Derivatives.

机构信息

College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Provincial Key Laboratory of Pathogenesis and Drug Research on Common Chronic Diseases, Guizhou Medical University, Guiyang, 550004, P. R. China.

Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, 550025, P. R. China.

出版信息

Chem Biodivers. 2022 Nov;19(11):e202200802. doi: 10.1002/cbdv.202200802. Epub 2022 Oct 10.

Abstract

Aiming to search for novel potential antifungal agents, forty 2H-chromene analogs were designed, synthesized and their antifungal activity against some typical plant pathogenic fungi were firstly evaluated. The in vitro antifungal bioassays showed that some of the target compounds exhibited comparable or better inhibition activities than the commercial agricultural fungicide hymexazol. Especially compound 1m displayed more promising fungicidal effect against Alternaria alternate (EC =9.9 μg/mL) and Botrytis cinerea (EC =9.4 μg/mL), which was significantly superior to hymexazol. Moreover, in vivo protective effects results also indicated that compound 1m had an excellent potential for further development as a new botanical pesticide.

摘要

为了寻找新型潜在抗真菌剂,设计、合成了 40 种 2H-色烯类似物,并首次评价了它们对一些典型植物病原真菌的抗真菌活性。体外抗真菌生物测定结果表明,部分目标化合物的抑制活性与商品化农业杀菌剂腈菌唑相当或更好。特别是化合物 1m 对番茄早疫病菌(EC=9.9μg/mL)和灰葡萄孢菌(EC=9.4μg/mL)显示出更有前途的杀菌效果,明显优于腈菌唑。此外,体内保护效果结果也表明,化合物 1m 具有作为新型植物源农药进一步开发的巨大潜力。

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