Synthesis, Crystal Structure and Herbicidal Activity of Aurone Derivatives

Pesticides based on natural products have attracted more and more attentions. They are low-toxic, readily degradable and low drug-resistant. This is an important field for developing new pesticides. Previous effords were mainly focused on developing new insecticides and bactericides. So there are few commercial herbicides originated from natural products. Aurones are natual product existing in fruits and flowers of certain plants. It was found that some of them show certain herbicidal activity. Herein, seventeen aurones derivatives were synthesized. X-ray single crystal diffraction analysis showed that the conformation of its double bond was Z. And these compounds were assayed for their inhibiting activity against Echinochloa crusgalli and B rassica cam pestris. The results indicate that they displayed modest inhabitation toward B rassica cam pestris, but bad toward Echinochloa crusgalli. Under 100 mu g/mL, inhibiting rate of compoud 15 on B rassica cam pestris was up to 88. 5%, and it reached to 81. 3% given by subsequent rescreening at 10 mu g/mL. Electronic property on ring A and lgP value of the whole molecular play a important role in maintainning its activiy. Compound 15 is a good leading structure for further optimization.