Institute of Experimental Botany AS CR, Prague, Czech Republic.
Bioorg Med Chem. 2010 Dec 1;18(23):8194-203. doi: 10.1016/j.bmc.2010.10.013. Epub 2010 Oct 29.
A series of 10 new pro-juvenoids (juvenogens, insect hormonogenic compounds, pro-drug-like agents) was synthesized using isomeric synthetic juvenoids (insect juvenile hormone analogs) and steroid molecules as patterns modifying parts of the complex hormonogenic molecules. In addition, several new synthons were prepared, which were required by the designed synthetic protocol to achieve the target molecules. These pro-juvenoids were subjected to the topical screening tests and to the drinking assays on the red firebug (Pyrrhocoris apterus), a convenient model laboratory phytophagous insect. Simple and efficient synthetic procedures for the preparation of the target pro-juvenoids and their synthons are presented. Furthermore, the biological activity of the pro-juvenoids in comparison with the activity of their parent juvenoids and that of several commercially available agents is demonstrated. Juvenoids and pro-juvenoids may replace toxic insecticides persistent in the insect pest control because they have no adverse effects on non-target organisms and/or human.
一系列 10 种新型亲幼激素（幼体激素，昆虫激素合成化合物，前药样化合物）是使用同系物合成幼体激素（昆虫保幼激素类似物）和甾体分子作为模式修饰复杂激素合成分子的一部分来合成的。此外，还制备了几个新的合成子，这些合成子是设计的合成方案中获得目标分子所必需的。对这些亲幼激素进行了局部筛选测试和对红蝽（Pyrrhocoris apterus）进行了口服测定，红蝽是一种方便的实验室植食性昆虫模型。介绍了制备目标亲幼激素及其合成子的简单高效的合成方法。此外，还证明了亲幼激素与亲幼激素及其几种市售制剂的活性相比的生物活性。幼体激素和前幼体激素可能取代在害虫防治中持续存在的有毒杀虫剂，因为它们对非目标生物和/或人类没有不良影响。
