Synthesis and Biological Activities of Novel Analogues of Phthalamide Containing Acylurea and Acylthiourea

doi:10.6023/cjoc201409005

Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (4): 882-889.DOI: 10.6023/cjoc201409005 Previous Articles Next Articles

ARTICLE

新型含酰基脲桥和硫脲桥的苯双酰胺类似物的合成及生物活性

陈有为, 万莹莹, 刘巧霞, 刘敬波, 熊丽霞, 于淑晶, 李正名

南开大学元素有机化学研究所元素有机化学国家重点实验室天津化学化工协同创新中心天津 300071

收稿日期:2014-09-05 修回日期:2014-10-30 发布日期:2014-11-27
通讯作者: 李正名 E-mail:nkzml@vip.163.com
基金资助:
国家重点基础研究发展计划(973计划, No. 2010CB126106)、国家自然科学基金(Nos. 31370039, 21272129)、国家科技攻关计划(No. 2011BAE06B05)、高等学校博士学科点专项科研基金(No. 20110031110017)资助项目.

Synthesis and Biological Activities of Novel Analogues of Phthalamide Containing Acylurea and Acylthiourea

Chen Youwei, Wan Yingying, Liu Qiaoxia, Liu Jingbo, Xiong Lixia, Yu Shujing, Li Zhengming

State Key Laboratory of Elemento-organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Research Institute of Elemento-organic Chemistry, Nankai University, Tianjin 300071

Received:2014-09-05 Revised:2014-10-30 Published:2014-11-27
Supported by:
Project supported by the National Basic Research Program of China (973 Program, No. 2010CB126106), the National Natural Science Foundation of China (Nos. 31370039, 21272129), the National Key Technologies R&D Program (No. 2011BAE06B05), and the Specialized Research Fund for the Doctorial Program of Higher Education (No. 20110031110017).

1. Synthesis and Biological Activities of Novel Analogues of Phthalamide Containing Acylurea and Acylthiourea.PDF(3195KB)

Abstract

In order to find novel and efficient insecticides targeting at the ryanodine receptor, a series of novel compounds containing acylurea and acylthiourea, referring to moieties of flubendiamide and diflubenzuron, were designed and synthesized. Their structures were characterized by ¹H NMR, HRMS and X-ray diffraction. The insectical activities showed that the introducing of acylurea and acylthiourea bridges decreased the acitivity. Compound 7d showed 50% activity at the concentration of 10 mg/L. In addtion, some structures showed moderate antifungal activities. Compound 8f displayed 75.0%, 87.5% and 84.6% antifungal activities against Botryosphaeria dothidea, Rhizoctonia cerealis and Fusarium fujikuroi.

Key words: flubendiamide, diflubenzuron, acylurea, acylthiourea, insecticidal activity, antifungal activity

Cite this article

Chen Youwei, Wan Yingying, Liu Qiaoxia, Liu Jingbo, Xiong Lixia, Yu Shujing, Li Zhengming. Synthesis and Biological Activities of Novel Analogues of Phthalamide Containing Acylurea and Acylthiourea[J]. Chin. J. Org. Chem., 2015, 35(4): 882-889.

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新型含酰基脲桥和硫脲桥的苯双酰胺类似物的合成及生物活性

Synthesis and Biological Activities of Novel Analogues of Phthalamide Containing Acylurea and Acylthiourea

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