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香豆素[8,7-e][1,3]恶嗪衍生物的微波辅助合成及其抗真菌活性

Microwave-assisted Synthesis and antifungal activity of coumarin[8,7-e][1,3]oxazine derivatives.

作者信息

Zhang Ming-Zhi, Zhang Rong-Rong, Yin Wen-Zheng, Yu Xiang, Zhang Ya-Ling, Liu Pin, Gu Yu-Cheng, Zhang Wei-Hua

机构信息

Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing, 210095, People's Republic of China.

Syngenta Jealott's Hill International Research Centre, Bracknell, Berkshire, RG42 6EY, UK.

出版信息

Mol Divers. 2016 Aug;20(3):611-8. doi: 10.1007/s11030-016-9662-2. Epub 2016 Feb 15.

DOI:10.1007/s11030-016-9662-2
PMID:26880591
Abstract

The synthesis of novel coumarin[8,7-e][1,3]oxazine derivatives through a microwave-assisted three-component one-pot Mannich reaction is described in this study. All the target compounds were evaluated in vitro for their antifungal activity against Botrytis cinerea, Colletotrichum capsici, Alternaria solani, Gibberella zeae, Rhizoctonia solani, and Alternaria mali. The preliminary bioassays showed that 5e, 5m, and 5s exhibited good antifungal activity and the most active compound was 5m with an [Formula: see text] value as low as 2.1 nM against Botrytis cinerea.

摘要

本研究描述了通过微波辅助的三组分一锅法曼尼希反应合成新型香豆素[8,7-e][1,3]恶嗪衍生物。对所有目标化合物进行了体外抗灰葡萄孢菌、辣椒炭疽病菌、番茄早疫病菌、禾谷镰刀菌、立枯丝核菌和苹果链格孢菌的抗真菌活性评估。初步生物测定表明，5e、5m和5s表现出良好的抗真菌活性，其中活性最高的化合物是5m，对灰葡萄孢菌的IC₅₀值低至2.1 nM。

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