酰基硫脲结构化合物具有多种生物活性.以噻二唑胺为原料,经卤代、肼解生成酰肼,再与不同取代的苯甲酰基异硫氰酸酯反应合成10 个新型含酰胺基硫脲结构的1,3,4-噻二唑衍生物(9a～9j).所有化合物的结构经IR、1 H NMR和HR-MS(ESI)表征.采用牛津杯法对其进行抗菌活性筛选,结果表明:9a～9j对哈氏弧菌活性存在不同程度的抑制作用,其中9d抗菌活性最好,抑菌圈直径为15.74±0.26 mm.
Abstract
Acyl thiourea compounds have various biological activities.Using thiadiazole as raw materi-al,they undergo halogenation and hydrazine hydrolysis to form hydrazides,which then react with dif-ferent substituted benzoyl isothiocyanates to synthesize 10 new 1,3,4-thiadiazole derivatives(9a～9j)with acyl thiourea structures.The structures of all compounds were characterized by IR,1 H NMR,and HR-MS(ESI).The Oxford Cup method was used to screen for its antibacterial activity,and the re-sults showed that 9a～9j had varying degrees of inhibitory effect on Vibrio harveyi activity.Among them,9d had the best antibacterial activity,with a diameter of 15.74±0.26 mm.
关键词
异硫氰酸酯/酰胺基硫脲结构/1,3,4-噻二唑衍生物/牛津杯法/抗菌活性/哈氏弧菌
Key words
isothiocyanate/amidothiourea structure/1,3,4-thiadiazole derivative/oxford cup method/antibacterial activity/vibrio harveyi
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