Te discovery of indoxacarb:oxadizines as a new class of pyrazoline-type insecticides

Stephen F McCann; Gary D Annis; Rafael Shapiro; David W Piotrowski; George P Lahm; Keith D Wing

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Te discovery of indoxacarb:oxadizines as a new class of pyrazoline-type insecticides

机译：茚虫威：恶二嗪类作为新型吡唑啉类杀虫剂的发现

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The evolution of the insecticidal pyrazoline moiety that was originally discovered in 1972 has led to the discovery of a new crop insecticide, indoxacarb, which is the first commercialized pyrazo-line-type sodium-channel blocker. Both monocydic and fused-tricyclic pyrazolines and pyridazines, as well as structurally related semicarbazones were examined prior to the discovery of analogous tricydic oxadiazines which had similarly high activity as well as favorable environmental dissipation rates and low toxicity to non-target organisms. The eventual leading candidate, DPX-JW062, was originally obtained as a racemic molecule, but a chiral synthesis was developed which produces material that is 50% ee in the insecticidal (—i--)-S-enantiomer (DPX-MP062, indoxacarb).

机译：最初在1972年发现的杀虫性吡唑啉部分的进化导致发现了一种新的农用杀虫剂茚虫威，这是第一种商业化的吡唑啉型钠通道阻滞剂。在发现类似的三甲基恶二恶嗪之前，先检查了单环和稠合三环吡唑啉和哒嗪以及结构相关的半咔唑酮，它们具有相似的高活性，有利的环境消散率和对非目标生物的低毒性。最终的领先候选物DPX-JW062最初是作为外消旋分子获得的，但是开发了一种手性合成方法，该方法产生的杀虫性（-i-）-S-对映异构体（DPX-MP062，茚虫威）的材料为ee的50％）。

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《Pest Management Science》 |2001年第2期|共12页
作者
Stephen F McCann; Gary D Annis; Rafael Shapiro; David W Piotrowski; George P Lahm; Keith D Wing;
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正文语种 eng
中图分类植物保护;
关键词
indoxacarb; oxadiazines; pyracoline insecticides; sodium-channel blockers; asymmetric synthesis;

机译：茚虫威;恶二嗪;吡咯啉类杀虫剂;钠通道阻滞剂;不对称合成;

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1. Te discovery of indoxacarb:oxadizines as a new class of pyrazoline-type insecticides [J] . Stephen F McCann, Gary D Annis, Rafael Shapiro, Pest Management Science . 2001,第2期

机译：茚虫威：恶二嗪类作为新型吡唑啉类杀虫剂的发现
2. A new class of insecticide for malaria vector control: evaluation of mosquito nets treated singly with indoxacarb (oxadiazine) or with a pyrethroid mixture against Anopheles gambiae and Culex quinquefasciatus [J] . Richard M. Oxborough, Raphael N’Guessan, Jovin Kitau, Malaria Journal . 2015,第S1期

机译：新型的用于控制疟疾的杀虫剂：分别用茚虫威（oxadiazine）或拟除虫菊酯混合物处理过的蚊帐，以对抗冈比亚按蚊和库蚊（Culex quinquefasciatus）
3. Point mutations at the local anesthetic receptor site modulate the state-dependent block of rat Na v1.4 sodium channels by pyrazoline-type insecticides. [J] . Silver KS, Soderlund DM Neurotoxicology . 2007,第3期

机译：局麻药受体点的点突变通过吡唑啉型杀虫剂调节大鼠Na v1.4钠通道的状态依赖性传导阻滞。
4. Synthesis and Biological Activity of Oxadiazine and Triazine Insecticides: The Discovery of Indoxacarb [C] . Stephen F. McCann, Gary D. Annis, Rafael Shapiro, American Chemical Society . 2002

机译：氧基嗪和三嗪杀虫剂的合成与生物活性：吲哚卡拉布的发现
5. Classifier design to improve pattern classification and knowledge discovery for imbalanced datasets. [D] . Wang, Kun. 2009

机译：分类器设计可改进模式分类和不平衡数据集的知识发现。
6. A new class of insecticide for malaria vector control: evaluation of mosquito nets treated singly with indoxacarb (oxadiazine) or with a pyrethroid mixture against Anopheles gambiae and Culex quinquefasciatus [O] . Richard M. Oxborough, Raphael N’Guessan, Jovin Kitau, 2015

机译：新型的用于控制疟疾的杀虫剂：分别用茚虫威（oxadiazine）或拟除虫菊酯混合物处理过的蚊帐以对抗冈比亚按蚊和库蚊（Culex quinquefasciatus）
7. A new class of insecticide for malaria vector control: evaluation of mosquito nets treated singly with indoxacarb (oxadiazine) or with a pyrethroid mixture against Anopheles gambiae and Culex quinquefasciatus [O] . Richard M. Oxborough, Raphael N’Guessan, Jovin Kitau, 2015

机译：新型的用于控制疟疾的杀虫剂：分别用茚虫威（oxadiazine）或拟除虫菊酯混合物处理过的蚊帐，以对抗冈比亚按蚊和库蚊（Culex quinquefasciatus）

Te discovery of indoxacarb:oxadizines as a new class of pyrazoline-type insecticides

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