Faculty of Education, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan.
J Agric Food Chem. 2011 Apr 13;59(7):2883-6. doi: 10.1021/jf103856c. Epub 2010 Nov 15.
Neonicotinoids are the newest of the five major classes of insecticides (the others are chlorinated hydrocarbons, organophosphorus compounds, methylcarbamates, and pyrethroids), and they make up approximately one-fourth of the world insecticide market. Nithiazine was the lead compound from Shell Development Co. in California later optimized by Shinzo Kagabu of Nihon Tokushu Noyaku Seizo to increase the potency and photostability, resulting in imidacloprid and thiacloprid. These discoveries are the basis for the International Award for Research in Agrochemicals of the American Chemical Society presented in 2010 to Professor Shinzo Kagabu. Five other neonicotinoids were added by others for the current set of seven commercial compounds. This symposium considers the progress in discovery and development of novel chemotype nicotinic insecticides with enhanced effectiveness, unique biological properties, and maximal safety. Chemorational approaches considered include physicochemical properties, metabolic activation and detoxification, and chemical and structural biology aspects potentially facilitating receptor structure-guided insecticide design.
新烟碱类杀虫剂是五大类杀虫剂（其他四类分别为氯化烃、有机磷化合物、氨基甲酸酯类和拟除虫菊酯类）中的最新一类，约占世界杀虫剂市场的四分之一。噻虫嗪是加利福尼亚州壳牌开发公司的先导化合物，后来由日本农药株式会社的 Shinzo Kagabu 进行优化，以提高其效力和光稳定性，从而得到了吡虫啉和噻虫啉。这些发现是美国化学学会颁发的 2010 年国际农业化学品研究奖的基础，该奖项授予 Shinzo Kagabu 教授。目前这一组 7 种商业化合物又增加了另外 5 种新烟碱类杀虫剂。本次专题讨论会考虑了新型化学型烟碱类杀虫剂的发现和开发进展，这些杀虫剂具有增强的有效性、独特的生物学特性和最大的安全性。所考虑的化学合理方法包括物理化学性质、代谢激活和解毒、以及化学和结构生物学方面，这些方面可能有助于基于受体结构的杀虫剂设计。
