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查尔酮衍生物的合成与抗真菌活性

Synthesis and antifungal activity of chalcone derivatives.

作者信息

Zheng Yuanyuan, Wang Xuesong, Gao Sumei, Ma Min, Ren Guiming, Liu Huabing, Chen Xiaohong

机构信息

a School of Physics and Chemistry, Xihua University , Chengdu 610039 , P.R. China.

出版信息

Nat Prod Res. 2015;29(19):1804-10. doi: 10.1080/14786419.2015.1007973. Epub 2015 Feb 12.

Abstract

In the present study, using chalcone as a lead compound, a series of its derivatives (compounds 1-30) were designed and synthesised. Their activity of anti-pathogenic fungi of plants has been evaluated. It is found that these compounds have good antifungal activity against Sclerotinia sclerotiorum, Helminthosprium maydis, Botrytis cinerea, Rhizoctonia solani and Gibberella zeae. Among them, the inhibition of growth for compound 30 against S. sclerotiorum showed 89.9%, with the median effective concentrations (EC50) of 15.4 μg mL(-1). The inhibition of growth for compounds 28, 29 and 30 at a concentration of 100 μg mL(-1) against H. maydis is 90.3%, 90.7% and 91.1%, with EC50 of 15.1, 18.3 and 18.1μg mL(-1), respectively.

摘要

在本研究中,以查尔酮为先导化合物,设计并合成了一系列其衍生物(化合物1 - 30)。评估了它们对植物病原真菌的活性。发现这些化合物对核盘菌、玉米大斑病菌、灰葡萄孢、立枯丝核菌和赤霉病菌具有良好的抗真菌活性。其中,化合物30对核盘菌的生长抑制率为89.9%,半数有效浓度(EC50)为15.4μg mL(-1)。化合物28、29和30在浓度为100μg mL(-1)时对玉米大斑病菌的生长抑制率分别为90.3%、90.7%和91.1%,EC50分别为15.1、18.3和18.1μg mL(-1)。

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