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天然产物及其衍生物、模拟物和合成类似物:在农用化学品发现中的作用。

Natural products, their derivatives, mimics and synthetic equivalents: role in agrochemical discovery.

作者信息

Sparks Thomas C, Hahn Donald R, Garizi Negar V

机构信息

Dow AgroSciences, Discovery Research, Indianapolis, IN, 46268, USA.

出版信息

Pest Manag Sci. 2017 Apr;73(4):700-715. doi: 10.1002/ps.4458. Epub 2016 Dec 17.

DOI:10.1002/ps.4458
PMID:27739147
Abstract

Natural products (NPs) have a long history as a source of, and inspiration for, novel agrochemicals. Many of the existing herbicides, fungicides, and insecticides have their origins in a wide range of NPs from a variety of sources. Owing to the changing needs of agriculture, shifts in pest spectrum, development of resistance, and evolving regulatory requirements, the need for new agrochemical tools remains as critical as ever. As such, NPs continue to be an important source of models and templates for the development of new agrochemicals, demonstrated by the fact that NP models exist for many of the pest control agents that were discovered by other means. Interestingly, there appear to be distinct differences in the success of different NP sources for different pesticide uses. Although a few microbial NPs have been important starting points in recent discoveries of some insecticidal agrochemicals, historically plant sources have contributed the most to the discovery of new insecticides. In contrast, fungi have been the most important NP sources for new fungicides. Like insecticides, plant-sourced NPs have made the largest contribution to herbicide discovery. Available data on 2014 global sales and numbers of compounds in each class of pesticides indicate that the overall impact of NPs to the discovery of herbicides has been relatively modest compared to the impact observed for fungicides and insecticides. However, as new sourcing and approaches to NP discovery evolve, the impact of NPs in all agrochemical arenas will continue to expand. © 2016 Society of Chemical Industry.

摘要

天然产物作为新型农用化学品的来源和灵感源泉,有着悠久的历史。许多现有的除草剂、杀菌剂和杀虫剂都源自各种来源的多种天然产物。由于农业需求的不断变化、害虫谱的转变、抗性的发展以及不断演变的监管要求,对新型农用化学工具的需求一如既往地至关重要。因此,天然产物仍然是新型农用化学品开发的重要模型和模板来源,许多通过其他方式发现的害虫防治剂都有天然产物模型这一事实就证明了这一点。有趣的是,不同天然产物来源在不同农药用途上的成功似乎存在明显差异。虽然一些微生物天然产物在近期某些杀虫农用化学品的发现中是重要的起点,但从历史上看,植物来源对新杀虫剂的发现贡献最大。相比之下,真菌一直是新型杀菌剂最重要的天然产物来源。与杀虫剂一样,植物来源的天然产物对除草剂发现的贡献最大。2014年各类农药的全球销售额和化合物数量的现有数据表明,与杀菌剂和杀虫剂相比,天然产物对除草剂发现的总体影响相对较小。然而,随着天然产物发现的新来源和方法不断发展,天然产物在所有农用化学品领域的影响将继续扩大。© 2016化学工业协会。

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