Design, Synthesis, and Insecticidal Activities of Novel Pyranoside Derivatives Targeting at Potential Second Calcium Channel IP₃ Receptor

详细信息    查看全文

• 作者：Changchun Wu ; Yuxin Li ; Ming Liu ; Jingbo Liu ; Xuewen Hua ; Dongkai Zhang ; Lixia Xiong ; Na Yang ; Baolei Wang and Zhengming Li
• 刊名：Chinese Journal of Chemistry
• 出版年：2016
• 出版时间：November, 2016
• 年：2016
• 卷：34
• 期：11
• 页码：1121-1128
• 全文大小：832K
• ISSN：1614-7065

文摘

In order to search for potent and environmental friendly insecticides with new modes of action, a series of pyranoside derivatives mimicking D-myo-inositol 1,4,5-trisphosphate (IP₃) were designed and synthesized according to the bioisosteric approach. The biological assay indicated that most of the new compounds showed moderate to good insecticidal activities against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella). Especially, compound 5g displayed 80% larvicidal activity against oriental armyworm at 50 mg/L. Meanwhile, 5a showed 100% and 70% larvicidal activities against diamondback moth at 50 and 25 mg/L, respectively. To further explore the mode of action, calcium imaging technique was applied to study the effects of 5a, 5g, and 5i on the intracellular calcium ion concentration ([Ca²⁺]_i) in central neurons isolated from Spodoptera exigua. The results indicated that the tested compounds released stored calcium ions from endoplasmic reticulum.