新型乙酰基取代的磺胺叔胺巯基唑类和磺胺叔胺氨基唑类化合物的设计合成及相关抗微生物作用研究  

Design,synthesis and relational biological researches of novel acetyl-contained sulfanilamide tertiary amine thiol azole compounds and sulfanilamide tertiary amine amino azole compounds

作　　者：冯丹阳 祝刘雪 杨士举 颜瑞 张慧珍[1] 王颖[1] FENG Dan-yang;ZHU Liu-xue;YANG Shi-ju;YAN Rui;ZHANG Hui-zhen;WANG Ying(School of Medicine,Linyi University,Linyi 276000,China)

机构地区：[1]临沂大学医学院,山东临沂276000

出　　处：《药学学报》2024年第12期3315-3324,共10页Acta Pharmaceutica Sinica

基　　金：山东省自然科学基金(ZR2020QB167);临沂大学本科一流课程(YLKC202318),临沂大学实验教学与实验技术研究项目(2023),临沂大学本科教学改革研究项目(2022)

摘　　要：磺胺类化合物作为重要的人工合成抗菌药,在抗感染领域发挥重要作用。本文基于磺胺类药物研发现状,突破磺胺经典结构,设计合成一系列乙酰基取代的磺胺叔胺巯基唑类和磺胺叔胺氨基唑类化合物,结构经^(1)H NMR、^(13)C NMR和HRMS确认。测试了新化合物的体外抗微生物活性,氨基三唑化合物7a的抗铜绿假单胞菌活性强于阳性对照药物诺氟沙星,且其对金黄色葡萄球菌的抑制活性接近于诺氟沙星。初步研究了化合物7a与小牛胸腺DNA的相互作用,并进行了化合物与DNA的对接实验研究。As an important synthetic antibacterial drug,sulfonamides play an important role in the antiinfection field.Based on the research and development status of sulfonamides,this paper broke the classical structure of sulfanilamide,and designed and synthesized a series of acetyl-contained sulfanilamide tertiary amine thiol azole compounds and sulfanilamide tertiary amine amino azole compounds.The structures were confirmed by ^(1)H NMR,^(13)C NMR and HRMS.The antimicrobial activity of synthesized compounds in vitro was tested.The antimicrobial activity of amino triazole compound 7a gave stronger activity against Pseudomonas aeruginosa than that of positive control drug norfloxacin,and its inhibitory activity against Staphylococcus aureus was close to that of norfloxacin.The interaction between compound 7a and calf thymus DNA was studied,and the docking experiment between this compound and DNA was also researched.

关 键 词：磺胺 叔胺 唑环 抗细菌 抗真菌 

分 类 号：R284[医药卫生—中药学]