Synthesis and biological activity of 2-(4,5-dihydroisoxazol-5-yl)-1,3,4-oxadiazoles

被引：26
作者：
Milinkevich, Kristin A. [1 ]
Yoo, Choong L. [1 ]
Sparks, Thomas C. [2 ]
Lorsbach, Beth A. [2 ]
Kurth, Mark J. [1 ]
机构：
[1] Univ Calif Davis, Dept Chem, Davis, CA 95616 USA
[2] Dow AgroSci LLC, Discovery R&D, Indianapolis, IN 46268 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 19期
基金：
美国国家科学基金会;
关键词：
1,3,4-Oxadiazole; Isoxazoline; Diheterocylce; Insecticidal activity; Small molecule library; 1,3-DIPOLAR CYCLOADDITION; LIBRARY; LEAD; 1,3,4-OXADIAZOLES; DESIGN;
D O I：
10.1016/j.bmcl.2009.07.139
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Acid hydrazides were coupled with acrylic acid derivatives and cyclodehydration gave 1,3,4-oxadiazoles. Lastly, in-situ nitrile oxide formation from aryl oximes treated with sodium hypochlorite, and subsequent 1,3-dipolar cycloaddition to the exomethylene moiety delivered 2-(4,5-dihydroisoxazol-5-yl)-1,3,4-oxadiazoles. This library was evaluated in a high-throughput screen at Dow AgroSciences. Several compounds were active against fungal pathogens and pest insects. (C) 2009 Published by Elsevier Ltd.
引用
收藏
页码：5796 / 5798
页数：3
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