三唑硫酮类化合物的合成与生物活性

方法]三唑硫酮类化合物具有广谱的生物活性。以2-氯烟酸为起始原料,经6步反应,设计并合成了一系列三唑硫酮类化合物,通过核磁等分析手段确定了其结构,并进行了生物活性测试。结论]共合成8个化合物,生测结果表明:该类化合物对白粉病具有较好的防治效果,并对其进行了初步的构效关系研究。构效关系表明:R2为吸电子取代基的化合物活性大于R2为给电子基取代的化合物。通过比较R1的不同取代位置,发现对位取代的化合物活性>邻位取代的化合物的活性>间位取代的化合物的活性。

Synthesis and Research of Biological Activity of Triazole Thiones

Methods] The compounds of triazole thiones showed a broad spectrum of bioactivities.A series of compounds were designed and synthesized from 2-chloronicotinic acid through six steps.The chemical structures of the target compounds were confirmed by NMR,and bioassay was carried out.Conclusions] Eight compounds were synthesized.The results indicated that this kind of compounds showed good activity against powdery mildew and the SAR of the compounds was studied.The activities of the compounds which R2 is electron-withdrawing groups are much better than that of electron-donating groups.Through comparing the substitution position of R1,it found that the activity order is p-substituted compounds > o-substituted compounds > m-substituted compounds.