新型含三唑及噻唑环的腙类化合物的合成及生物活性研究

Synthesis and Biological Activity of Some Novel Hydrazones Containing Triazole and Thiazole

为寻找具有医用或农用生物活性的新颖化合物,以对氯苯胺为起始原料,经由四步反应,制得1-对氯苯基-5-甲基-1,2,3-三唑-4-乙酮缩氨基硫脲(3),随后中间体3与ω-溴代芳基乙酮在无水乙醇中回流或在超声波辐射下反应,得到了一系列新型N-(1-对氯苯基-5-甲基-1,2,3-三唑-4-乙酰基)-N′-(4-芳基-噻唑-2-基)腙类化合物.用1H NMR,MS谱和元素分析对所有化合物进行了结构表征.初步生物活性测试表明,化合物4d和4e表现出一定的生物活性.

In order to find novel compounds with medical or agricultural bioactivity,1-chlorophenyl-5-methyl-1,2,3-triazol-4-ethanonethiosemicarbazone was obtained from p-chlorophenylamine as starting materials by four-step reaction,followed by the reaction of intermediate 3 with ω-bromoacetophenone under reflux con-dition or ultrasonic irradiation to afford a series of N-（1-p-chlorophenyl-5-methyl-1,2,3-triazole-4-acetyl）-N＇-（4-aryl-thiazol-2-yl）-hydrazones.The structures of all compounds were characterized by elemental analy-sis,1H NMR and MS techniques.The results of preliminary bioactivity tests indicated that compounds 4d and 4e possess certain biological activities.