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无溶剂合成及砜脲苯并噻唑啉的保护剂活性。

Solvent-Free Synthesis and Safener Activity of Sulfonylurea Benzothiazolines.

机构信息

Department of Applied Chemistry, College of Science, Northeast Agricultural University, Harbin 150030, China.

出版信息

Molecules. 2017 Sep 22;22(10):1601. doi: 10.3390/molecules22101601.

Abstract

A series of novel sulfonylurea benzothiazolines was designed by splicing active groups and bioisosterism. A solvent-free synthetic route was developed for the sulfonylurea benzothiazoline derivatives via the cyclization and carbamylation. All compounds were characterized by IR, ¹H-NMR, C-NMR, HRMS. The biological activity tests indicated the compounds could protect maize against the injury caused by chlorsulfuron to some extent. The molecular docking result showed that the new compound competed with chlorsulfuron to bind with the herbicide target enzyme active site to attain detoxification.

摘要

设计了一系列新型磺酰脲苯并噻唑啉,通过拼接活性基团和生物等排体。通过环化和氨甲酰化,开发了一种无溶剂合成磺酰脲苯并噻唑啉衍生物的路线。所有化合物均通过 IR、¹H-NMR、C-NMR、HRMS 进行了表征。生物活性测试表明,这些化合物在一定程度上可以保护玉米免受氯磺隆的伤害。分子对接结果表明,新化合物与氯磺隆竞争,与除草剂靶酶活性位点结合以达到解毒的目的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f4e/6151413/c05f53cb6bcb/molecules-22-01601-sch001.jpg

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