Chinese Journal of Organic Chemistry >
Synthesis and Biological Activity of 2-Cyanobenzenesulfonylurea Derivatives
Received date: 2018-04-10
Revised date: 2018-05-24
Online published: 2018-06-07
Supported by
Project supported by the Fundamental Research Funds for the Central Universities (No. 2682016CX104) and the National Natural Scinece Foundation of China (No. 21272129).
In order to study the multi-bioactivity of sulfonylurea derivatives, fifteen novel 2-cyano-6-chlorobenzenesul-fonylureas were designed and synthesized according to pharmacophore-combination and bioisosterism strategy, based on the chlorsulfuron and tritosulfuron structure frameworks. Their structures were confirmed by 1H NMR, 13C NMR and HRMS. The preliminary bioactivity test indicated that some of the title compounds had excellent in vitro antibacterial activity and insecticidal activity. For example, at the concentration of 50 mg·L-1, the antifungal activities of 5c, 5f and 5g against Physalospora piricola were 80.3%, 80.3% and 83.6% respectively. 5j exhibted 50% larvicidal activity against Mythimna separate Walker at the dosage of 50 mg·L-1. At the concentration of 0.1 mg·L-1, 5a and 5b showed 100% and 50% insecticidal activity against Culex pipiens pallens, respectively better than that of the control flubendiamide (20%). At an even low concentration of 0.01 mg·L-1, 5a had 70% larvicidal activity, and the LC50 value was 0.0023 mg·L-1.
Chen Wei , Li Yuxin , Li Yonghong , Yu Shujing , Xiong Lixia , Li Zhengming . Synthesis and Biological Activity of 2-Cyanobenzenesulfonylurea Derivatives[J]. Chinese Journal of Organic Chemistry, 2018 , 38(10) : 2747 -2753 . DOI: 10.6023/cjoc201804019
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