4-(硫)色满酮Schiff碱衍生物的合成与生物活性研究

Synthesis and Bioactivity of Schiff Bases of 4-(Thio)chromanones

为寻找具有更高活性的农药先导化合物。以3-溴丙酸和取代苯(硫)酚为起始原料,经醚化、环合、加成等反应合成了6个未见文献报道的4-(硫)色满酮Schiff碱类化合物(7a-7f),其结构经IR、^(1)H NMR和^(13)C NMR确证。分别采用油菜平皿法和菌丝生长速率法测试了这些化合物的除草活性和抑菌活性。结果表明,目标化合物在50~200 mg/L下均具有一定的除草和抑菌活性。其中,7a~7f对刺苋根的抑制率达到80%以上,7b对小麦冠腐病菌的抑制率达到85%以上。

In order to find out novel pesticide lead compounds with higher activity,six novel schiff bases of 4-(thio)chromanones were synthesized with 3-bromopropionic acid and substituted(thio)phenol as raw material by reactions of etherification,cyclization and addition.Their structures were confirmed by IR,^(1)H NMR,and ^(13)C NMR.Their herbicidal and bacteriostatic activity were determined by brassica napus plate method and mycelium growth rate method respectively.The results showed that the title compounds displayed herbicidal activities and fungicidal activities in some degree at the concentration of 50~200 mg/L.Among them,the inhibition rate of compound 7a~7f on Amaranthus spinosus L.root was above 80%,and the inhibition rate of 7b against Fusarium pseudograminearum was above 85%.