Discovery of novel 3‐{[(5,5‐dimethyl‐4,5‐dihydroisoxazol‐3‐yl)sulfonyl]methyl}benzo[d]isoxazole analogs as promising very long chain fatty acids inhibitors,Journal of Heterocyclic Chemistry

当前位置： X-MOL 学术 › J. Heterocycl. Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Discovery of novel 3‐{[(5,5‐dimethyl‐4,5‐dihydroisoxazol‐3‐yl)sulfonyl]methyl}benzo[d]isoxazole analogs as promising very long chain fatty acids inhibitors
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-10-01 , DOI: 10.1002/jhet.4162
Jian Lin _{1,

2} , Yitao Li ₁ , Xiaoyun Hu ₁ , Weilin Chi ₁ , Shuiming Zeng ₁ , Junxing Xu ₁

Affiliation

Very long chain fatty acids (VLCFAs) are one of the most principal and promising targets for herbicides discovery. In order to explore and find novel VLCFAs inhibitors with higher herbicidal activity and improved crop safety, a variety of new 3‐{[(5,5‐dimethyl‐4,5‐dihydroisoxazol‐3‐yl)sulfonyl]methyl}benzo[d]isoxazole derivatives were reasonably designed and synthesized. The results of greenhouse experiments indicated that several compounds exhibited good herbicidal activity against Digitaria sanguinalis, Echinochloa crus‐galli, and Setaria faberii at rates of 150 g ai/ha. Compounds g4 and h1 displayed promising herbicidal activity against D sanguinalis and E crus‐galli at rates of 75 g ai/ha, which is better than commercial pyroxasulfone and S‐metolachlor. Moreover, compound h1 displayed higher activity against E crus‐galli, D sanguinalis, and S faberii than pyroxasulfone and S‐metolachlor even at a rate of 37.5 and 18.75 g ai/ha. Furthermore, both of the compounds g4 and h1 were much safer to these tested crops, especially to rice, wheat and rape, at the rate of 150 g ai/ha than pyroxasulfone. Therefore, h1 may act as a new lead structure for novel herbicides discovery.

中文翻译：

发现新的3-{[（（5,5-二甲基-4,5-二氢异恶唑-3-基）磺酰基]甲基]苯并[d]异恶唑类似物作为很有前途的长链脂肪酸抑制剂

超长链脂肪酸（VLCFA）是除草剂发现的最主要和最有希望的目标之一。为了探索和发现具有更高除草活性和改善作物安全性的新型VLCFAs抑制剂，使用了多种新的3-{[（5,5-二甲基-4-4,5-二氢异恶唑-3-基）磺酰基]甲基}苯并[d]对]异恶唑衍生物进行了合理的设计和合成。温室试验的结果表明，几种化合物以150 g ai / ha的速率对Digitaria sanguinalis，Echinochloa crus-galli和Setaria faberii表现出良好的除草活性。化合物g4和h1对D血红蛋白和C. crus-galli表现出有希望的除草活性剂量为75 g ai / ha，优于商业吡pyr砜和S-异丙甲草胺。此外，化合物H1显示对更高的活性Ë稗，d马唐和小号大狗尾草甚至在37.5 18.75 g的速度比，pyroxasulfone与S-异丙甲草胺成分/公顷。此外，化合物g4和h1对这些试验作物，特别是对水稻，小麦和油菜的安全性均比吡ox砜高150 g ai / ha。因此，h1可以作为发现新型除草剂的新先导结构。

更新日期：2020-10-01

点击分享查看原文

点击收藏

阅读更多本刊新发论文本刊介绍/投稿指南