Laboratory of Pharmaceutical Design and Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, China.
Bioorg Med Chem Lett. 2011 Apr 1;21(7):1974-7. doi: 10.1016/j.bmcl.2011.02.031. Epub 2011 Feb 13.
In continuation of our program aimed at the discovery and development of natural products-based insecticidal agents, twelve 28-acyloxy derivatives of toosendanin (2a-l) were semisynthesized and preliminarily evaluated their activity against the pre-third-instar larvae of Mythimna separata Walker in vivo at the concentration of 1mg/mL. Some compounds exhibited the potent insecticidal activity. Especially compounds 2c and 2j displayed the more promising insecticidal activity than their natural precursor, toosendanin, a commercial insecticide derived from Melia azedarach at 1mg/mL. In general, it indicated that the butanoyloxy or phenylacryloyloxy moiety at the 28-position of toosendanin was essential for the insecticidal activity.
在我们继续进行旨在发现和开发基于天然产物的杀虫剂的项目中，我们半合成了十二种 28-酰氧基托品酮（2a-l）衍生物，并在 1mg/mL 的浓度下初步评估了它们对三化螟幼虫的活性。一些化合物表现出很强的杀虫活性。特别是化合物 2c 和 2j 的杀虫活性比其天然前体、从苦楝树中提取的商业杀虫剂托品酮更为显著。总的来说，这表明托品酮 28 位上的丁酰氧基或苯丙烯酰氧基部分对于杀虫活性是必需的。
