State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Company Ltd. , Shenyang 110021, China.
J Agric Food Chem. 2016 Jan 13;64(1):45-51. doi: 10.1021/jf5054707. Epub 2015 Jan 5.
Intensive competition of intellectual property, easy development of agrochemical resistance, and stricter regulations of environmental concerns make the successful rate for agrochemical discovery extremely lower using traditional agrochemical discovery methods. Therefore, there is an urgent need to find a novel approach to guide agrochemical discovery with high efficiency to quickly keep pace with the changing market. On the basis of these situations, here we summarize the intermediate derivatization method (IDM) between conventional methods in agrochemicals and novel ones in pharmaceuticals. This method is relatively efficient with short time in discovery phase, reduced cost, especially good innovated structure, and better performance. In this paper, we summarize and illustrate "what is the IDM" and "why to use" and "how to use" it to accelerate the discovery of new biologically active molecules, focusing on agrochemicals. Furthermore, we display several research projects in our novel agrochemical discovery programs with improved success rate under guidance of this strategy in recent years.
知识产权的激烈竞争、农用化学品抗药性的容易发展以及对环境问题的更严格规定，使得使用传统农用化学品发现方法的农用化学品发现的成功率极低。因此，迫切需要找到一种新的方法来指导农用化学品的发现，以高效率快速跟上不断变化的市场。基于这些情况，我们在这里总结了介于传统农用化学品方法和新型药物方法之间的中间体衍生化方法 (IDM)。该方法在发现阶段时间短、成本低、结构新颖性好、性能好，相对高效。本文总结并说明了“什么是 IDM”、“为什么要使用”以及“如何使用”它来加速新的具有生物活性的分子的发现，重点是农用化学品。此外，我们还展示了近年来在我们的新型农用化学品发现计划中，在该策略指导下，几个提高成功率的研究项目。
