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

…, CL Yoo, TC Sparks, BA Lorsbach, MJ Kurth

Index: Milinkevich, Kristin A.; Yoo, Choong L.; Sparks, Thomas C.; Lorsbach, Beth A.; Kurth, Mark J. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 19 p. 5796 - 5798

Full Text: HTML

Citation Number: 23

Abstract

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 ...