新型硫脲聚合物的合成及其生物活性研究

【作者】 吴再坤；

【导师】 钟宏；

【作者基本信息】 中南大学 ， 生物化工， 2007， 硕士

【摘要】 本文以酰基硫脲类化合物的结构为先导，根据该类化合物具有的良好生物活性，结合高分子与药物合成设计的相关方法，分别以对苯二甲酰氯和1,4-丁二醇为起始原料合成出了1,4-苯二羰基硫脲和1,4-丁二氧羰基硫脲两个系列聚合物。并且在聚合物中引入了硫脲、二苯醚和苯氧乙酸等活性基团，对聚合物的结构进行了改性。并通过对1,4-苯二羰基二异硫氰酸酯这一新类中间体的制备及其与二胺的聚合加成反应，开辟了硫脲聚合物的新合成方法，并利用红外光谱、核磁共振对所合成的聚合物进行了结构表征。采用农药生物活性测定的标准操作程序，测试了所合成聚合物的除草活性，对作物的安全性能以及抗菌活性。根据剂效曲线发现大多数聚合物的抑制率均随浓度的增大而增大，其中PBDT-b，PBDT-e和PTDT-a对单子叶稗草和双子叶作物黄瓜分别表现出不同程度的抑制活性，而对单子叶作物水稻则表现出良好的促进作用。通过测定聚合物的抑菌性能，发现所合成聚合物的抑菌活性均很小。通过对聚合物的结构与生物活性之间的定性研究，论文揭示了酰基和氨基甲酸酯类硫脲聚合物潜在的生物活性，探讨了硫脲类聚合物的新应用，从而为高效、低毒的硫脲类微胶囊农药囊材的合成与选择提供了现实依据。更多还原

【Abstract】 According to the structure and predominant bioactivity of acyl thiourea polymers, and combining the correlative method of medicine synthesizing and macromolecule designing in this thesis, two series of thourea polymers which contain a 1,4-benzenedicarbonyl or 1,4-butyldioxylcarbonyl thiourea group were synthesized with 1,4-benzenedicarbonly dichloride or 1,4-butanediol as original material. Those allied activity groups such as Thiourea, diphenylether and phenoxyacetic groups etal were imported into polymers, and the structure of polymer was modified. A new kind of synthetical method about thiourea polymer was invented by synthesizing a new style of intermediate named dicarbonyl diisorhodanate and making it aggregate with diamine compounds. The structure of compounds prepared was characterized with infrared spectrum and nuclear magnetic resonance.The bioassays, safety for corp and antibacterial capability of polymers prepared were carried out according to the standard operation procedure of pesticide bioassay. And Dose-response graphs showed that the inhibiting rate about most of polymers increased with concentration. PBDT-b, PBDT-e and PTDT-a showed different grade of inhibiting activity againsting monocotyledon weeds such as Echinochloa crusgalli and dicotyledon corp such as cucumber, but showed predominant promoting activity againsting monocotyledon corp such as Oryza sativa L. The result obtained from the experiment of testing the antibacterial capability showed that all polymers prepared had little antibactical activity.In the light of qualitative study on the relationship between chemical structure and Bioactivity, the thesis outlined the potential bioactivity of acyl and carbamate thiourea polymers, discussed the new appliance of thiourea polymers. Hence, it had provided practical gist for synthesis of microcapsule membrane which will be applied in thiourea microcasuple pesticide with the character of high effect and low toxicity.更多还原