双取代硫脲的连续反应合成及生物活性测试  

Synthesis and Bioactivities of Diaryl-substituted Thiourea by Continuous Reaction

作　　者：秦永其 秦悦笙 褚盼盼[3] Qin Yongqi;Qin Yuesheng;Chu Panpan(Lyuliang Key Laboratory of Comprehensive Utilization of Organic Waste Resources,Lyuliang 033001,China;Department of Chemistry and Chemical Engineering,Lyuliang University,Lyuliang 033001,China;Department of Biology,Lyuliang University,Lyuliang 033001,China;Department of Traditional Chinese Medicine,Inner Mongolia Medical University,Huhehot 010000,China)

机构地区：[1]吕梁有机废物资源综合利用吕梁市重点实验室,山西吕梁033001 [2]吕梁学院化学化工系,山西吕梁033001 [3]吕梁学院生物系,山西吕梁033001 [4]内蒙古医科大学中医系,内蒙古呼和浩特010000

出　　处：《山东化工》2024年第4期4-6,共3页Shandong Chemical Industry

基　　金：山西省教育厅教学改革项目(J2021724);吕梁有机废弃物资源化综合利用重点实验室(ZDSYS2018056);吕梁市重点研发重点项目(2021GXYF-1-19);重大疾病创新药物山西省重点实验室开放基金(2021sxcxyw11);超重力化工过程山西省重点实验室开放基金项目(CZL2020-04)资助。

摘　　要：以取代苯胺为原料,经过连续加料的方式,合成了9个二苯基硫脲衍生物,通过元素分析、MS、IR、以及^(1)H NMR对系列化合物进行了结构表征。同时,采用纸张琼脂扩散法测试了9种目标化合物对金黄色葡萄球菌和大肠杆菌的生物活性抑制情况,总结了不同浓度和不同取代基的目标产物对金黄色葡萄球菌和大肠杆菌的抑菌情况的影响。测试结果表明,含氯取代基的化合物对金黄色葡萄球菌的抑制作用有利,具体影响规律:邻氯>对氯>2,4-二氯苯基,而含F化合物对大肠杆菌的抑制作用有利。化合物1a对金黄色葡萄球菌的抑菌圈直径达到1.9 cm。这些参数为高活性硫脲类化合物的合成和筛选提供了依据。Nine diphenylthiourea derivative were synthesized from substituted aniline by means of continuous feeding.Their structures were characterized by Elemental analysis,MS,IR and ^(1)H NMR.Meanwhile,Their biological activities have been measured by paper agar diffusion method.Target compounds were tested for the bioactivity of S.aureus and E.coli.Biological activities are affected by different substituents and concentrations.The test results showed that Compounds of chloro-substituent are good for Antibacterial activity of S.aureus.Specific impacts:o-Cl>p-Cl>2,4-two Cl.F-containing compounds are s.beneficial s.to biological activities of E.coli.The diameter of the inhibition zone of the compound 1a was 1.9 cm against S.aureus.These parameters will provide a scientific data for screening and making high activity thiourea compounds.

关 键 词：连续加料 合成 硫脲衍生物 生物活性 

分 类 号：TQ450.1[化学工程—农药化工]