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首页> 外文期刊>Journal of Agricultural and Food Chemistry >Design, Synthesis, and 3D-QSAR Analysis of Novel 1,3,4-Oxadiazol-2(3H)-ones as Protoporphyrinogen Oxidase Inhibitors
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Design, Synthesis, and 3D-QSAR Analysis of Novel 1,3,4-Oxadiazol-2(3H)-ones as Protoporphyrinogen Oxidase Inhibitors

机译：新型1,3,4-Oxadiazol-2（3H）-one作为原卟啉原氧化酶抑制剂的设计，合成和3D-QSAR分析

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摘要

Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) has been identified as one of the most significant action targets for a large chemically diverse family of herbicides that exhibit some interesting characteristics, such as low use rate, low toxicity to mammals, and low environmental impact. As a continuation of research work on the development of new PPO inhibitors, some benzothiazole analogues of oxadiargyl, an important PPO-inhibiting commercial herbicide, were designed and synthesized by ring-closing of the substituents at the C-4 and C-5 positions. The bioassay results indicated that the series 8, 9, and 10 have good PPO inhibition activity with k_i values ranging from 0.25 to 18.63 μM. Most interestingly, 91, ethyl 2-((5-(5-tert-butyl-2-oxo-1,3,4-oxadiazol-2(3H)-yl)-6r fluorobenzothiazol-2-yl)sulfanyl) propanoate, was identified as the most promising candidate due to its high PPO inhibition effect (K_i = 1.42 μM) and broad spectrum postemergence herbicidal activity at the concentration of 37.5 g of ai/ha.
机译：原卟啉原氧化酶（PPO，EC 1.3.3.4）已被确定为化学除草剂家族中最重要的作用目标之一，这些除草剂具有一些有趣的特征，例如使用率低，对哺乳动物的毒性低以及对环境的影响小。 。作为开发新的PPO抑制剂的研究工作的继续，通过在C-4和C-5位上的取代基闭环设计并合成了一些重要的PPO抑制性除草剂恶二argyl的苯并噻唑类似物。生物测定结果表明，系列8、9和10具有良好的PPO抑制活性，k_i值为0.25至18.63μM。最有趣的是，91，2-（（5-（5-叔丁基-2-氧代-1,3,4-恶二唑-2（3H）-基）-6r氟苯并噻唑-2-基）硫烷基）丙酸酯，由于其高PPO抑制作用（K_i = 1.42μM）和在37.5 g ai / ha的浓度下具有广谱的芽后除草活性，因此被确定为最有前途的候选者。

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