Design, synthesis and bioactivity evaluation of novel acylthiourea derivatives of cantharidin

• 作 者: Mei-JuanWang[1]Wen-QunLi[1]XiangNan[1]Ying-QianLiu[1]KeduoQian[2]Guan-FangHu[3]Hai-TaoYu[3]Kuo-HsiungLee[2]
• 机 构: School of Pharmacy,Lanzhou University,Lanzhou 730000,PR China
• 出 处: 第十三届全国农药学教学科研研讨会
• 发表日期: 2013年期

　　In an attempt to find the biorational pesticides, a series of novel acylthiourea derivatives of cantharidin (1) were designed, synthesized and evaluated for their bioactivity against T.Cinnabarinus and B.brassicae.All the new compounds showed potent acaricidal activity against T.Cinnabarinus with LCs0 values ranging from 0.703 to 2.934 mmol/L.Moreover, these compounds displayed better acaricidal activity against T.Cinnabarinus than insecticidal activity against B.brassicae.Based on the observed bioactivities, the structure-activity relationship (SAR) of these analogs was also discussed.The present work indicated that cantharidin derivatives can be used as potential leads for developing novel insecticides and acaricides.