论文部分内容阅读
目的:利用点击化学反应合成四氮唑类化合物,寻找温和的反应条件。对合成的四氮唑类化合物进行体外抑菌活性研究,以期发现抑菌活性化合物并初步研究其构效关系。方法:以氰基类化合物和叠氮钠为原料,溴化锌为催化剂,通过点击化学反应合成一类四氮唑结构化合物并研究其合成工艺条件的优化。利用微量二倍稀释法对合成的四氮唑类化合物进行体外抑菌活性测试。结果:利用所得到的优化点击化学反应条件合成了11个四氮唑类化合物,并发现化合物2h具有广谱抑菌活性。结论:优化后的点击化学反应条件温和,后处理方便,产率较高。抑菌活性和构效关系研究为后续的四氮唑类化合物抑菌活性研究工作提供了一定的基础。
OBJECTIVE: To synthesize tetrazolium compounds by click chemical reaction and to search for mild reaction conditions. The antibacterial activity of the synthesized tetrazolium compounds in vitro was studied in order to find the antibacterial compounds and to study their structure-activity relationship. Methods: A series of tetrazolium compounds were synthesized by click chemical reaction using cyano compounds and sodium azide as raw materials and zinc bromide as catalyst, and the optimization of the synthesis process was studied. The in vitro antibacterial activity of the synthesized tetrazolium compounds was tested by using the method of two times dilution. Results: Eleven tetrazole compounds were synthesized using the optimized conditions of click chemistry. Compound 2h was also found to have a broad spectrum antibacterial activity. Conclusion: The optimized click chemistry reaction conditions are mild, the post-treatment is convenient and the yield is high. Antibacterial activity and structure-activity relationship studies for the follow-up of the antibacterial activity of tetrazole compounds provide a basis for the study.