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首页> 外文期刊>Journal of Agricultural and Food Chemistry >Design, Herbicidal Activity, and QSAR Analysis of Cycloalka[d]quinazoline-2,4-dione-Benzoxazinones as Protoporphyrinogen IX Oxidase Inhibitors
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Design, Herbicidal Activity, and QSAR Analysis of Cycloalka[d]quinazoline-2,4-dione-Benzoxazinones as Protoporphyrinogen IX Oxidase Inhibitors

机译：Cycloka [D]喹唑啉-2,4-二酮 - 苯并恶嗪作为原子卟啉IX氧化酶抑制剂的设计，除草活性和QSAR分析

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摘要

In continuation of our search for potent protoporphyrinogen IX coddase (PPO, EC 1.3.3.4) inhibitors, we designed and synthesized a series of novel herbicidal cycloalka[d]quinazoline-2,4-dione-benzoxazinones. The bioassay results of these synthesized compounds indicated that most of the compounds exhibited very strong Nicotiana tabacum PPO (NtPPO) inhibition activity. More than half of the 37 synthesized compounds displayed over 80% control of all three tested broadleaf weeds at 37.5-150 g ai/ha by postemergent application, and a majority of them showed no phytotoxicity toward at least one kind of crop at 150 g ai/ha. Promisingly, 17i (K-i = 6.7 nM) was 6 and 4 times more potent than flumioxazin (K-i = 46 nM) and trifludimoxazin (K-i, = 31 nM), respectively. Moreover, 17i displayed excellent, broad-spectrum herbicidal activity, even at levels as low as 37.5 g ai/ha, and it was determined to be safe for wheat at 150 g ai/ha in postemergent application, indicating the great potential for 17i development as a herbicide for weed control in wheat fields.
机译：继续我们寻求有效的原子卟啉IX Coddase（PPO，EC 1.3.3.4）抑制剂，我们设计和合成了一系列新的除草剂Cycloalka [D]喹唑啉-2,4-二酮 - 苯并恶嗪。这些合成化合物的生物测定结果表明，大多数化合物表现出非常强烈的尼古特塔巴哈克PPO（NTPPO）抑制活性。 37种合成化合物中的一半以上显示了37.5-150克AI /公顷的所有三个测试的阔叶杂草的80％以上的控制，其中大多数朝向150g AI的至少一种作物表现出植物毒性/哈。承诺，17i（K-I = 6.7nm）分别比氟哌嗪（K-I = 46nm）和三氟胺毒素（K-1，= 31nm）更高的效力为6和4倍。此外，17i显示出优异的广谱除草活性，即使在低至37.5g AI / ha的水平下，它也被确定为在后宫期间的150g AI / ha处的小麦安全，表明17i开发的巨大潜力作为麦田杂草控制的除草剂。

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