异噁唑衍生物的合成及其抗菌活性研究  

Synthesis and antibacterial activity of derivatives containing isoxazoline

作　　者：张存彦[1] 刘登科[2] 孙长海[1] 刘默[2] 刘威[2] 

机构地区：[1]天津红日药业股份有限公司,天津301700 [2]天津药物研究院,天津300193

出　　处：《现代药物与临床》2012年第1期14-18,共5页Drugs & Clinic

基　　金：天津市科委基础科学重点资助项目(033801911)

摘　　要：目的设计并合成异噁唑衍生物,并对其体外抗菌活性进行了初步评价。方法以3,4-二氟苯甲醛、盐酸羟胺为起始原料,经多步反应合成目标化合物。以利奈唑胺为阳性对照药,对目标化合物的抗菌活性进行评价。结果合成了9个新化合物,其结构经1H-NMR、MS确证,体外活性测试结果显示,有1个化合物有显著的抗菌活性,与利奈唑胺相当。结论体外活性试验表明,含异唑的所制备化合物作为新型的抗菌剂,其构效关系值得进一步研究。Objective To design and synthesize antibacterial derivatives containing isoxazoline, and to evaluate their antibacterial activities. Methods The target compounds were synthesized with the starting material 3, 4-difluoro-benzaldehy with hydroxylamine hydrochloride. And their antibacterial activities have been tested in vitro with linezolide as positive control. Results Nine target compounds were synthesized and their structures were confirmed by 1H-NMR, MS. The pharmacological tests showed that one of the tested compounds exhibited novel antibacterial activity compared with linezolide. Conclusion The structure-activity relationships of isoxazoline derivatives, as a novel antibaterial type, should be further investigated.

关 键 词：异噁唑 衍生物 3 4-二氟苯甲醛 利奈唑胺 抗菌活性 

分 类 号：R914[医药卫生—药物化学]