In order to develop new biorational pesticides and clarify the potential structural factors needed for the biological activity of celangulin-V analogues, thirty novel nitrogenous derivatives were designed and synthesized. The single crystal structure of celangulin-V is reported for the first time and provides a more accurate structure than that previously reported. The structures of all the new derivatives were confirmed by either NMR or ESI-MSn analysis. Insecticidal activities of these compounds were tested against the third-instar larvae of Mythimna separata. One derivative (1-6) showed higher insecticidal activity than celangulin-V, with a KD50 of 231.2 microg.g(-1), while two compounds (2-13 and 2-14) exhibited lower insecticidal activities; the others revealed no activity at a concentration of 20 mg mL(-1). The results support the view that celangulin-V has the potential to be a lead structure of semi-synthetic green insecticides.

中文翻译：

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新的天蓝蛋白-V含氮衍生物的合成及杀虫活性。

为了开发新的具有生物合理性的农药并弄清天蓝素-V类似物的生物活性所需的潜在结构因素，设计并合成了三十种新型含氮衍生物。首次报道了天蓝蛋白-V的单晶结构，并且比先前报道的结构提供了更准确的结构。所有新衍生物的结构均通过NMR或ESI-MSn分析确认。测试了这些化合物对Mythimna separata的三龄幼虫的杀虫活性。一种衍生物（1-6）显示出比celangulin-V更高的杀虫活性，KD50为231.2 microg.g（-1），而两种化合物（2-13和2-14）显示出较低的杀虫活性。其他人在浓度为20 mg mL（-1）时无活性。