吡啶联异噁唑啉类杂环衍生物的合成及生物活性

Synthesis and Biological Activity of Pyridinyl-4,5-2H-isoxazole Heterocyclic Derivatives

摘要:

以2-氯-5-氯甲基吡啶为原料，合成了12个吡啶联异噁唑啉类杂环衍生物（9a~l），其结构经1HNMR、13CNMR、MS及IR表征。体外抗菌活性测试结果表明：所得目标化合物对金黄色葡萄球菌(ATCC25923)、肺炎链球菌(ATCC49619)和粪肠球菌(ATCC29212)都有一定的抑制作用，其中化合物9f和9l的抗菌效果最佳；体外驱虫活性测试结果表明：目标化合物都有一定的驱虫效果，其中化合物9a-b和9g-h的驱虫效果明显强于阿苯达唑。本实验为开发新型抗菌及驱虫药物提供初步依据，化合物活性的进一步优化及作用方式的确认等研究工作正在进行中。

Abstract:

Twelve Pyridinyl-4,5-2H-isoxazole Heterocyclic derivatives were synthesized from 2-chloro-5-chloromethylpyridine and their structures were characterized by 1HNMR, 13CNMR, MS and IR. The antibacterial activities results indicated all of them exhibited potent activities against Staphylococcus aureus (ATCC25923), Streptococcus pneumonia (ATCC49619) and Enterococcus faecalis (ATCC29212). Among of them, compound 9f and 9l showed the best activities. All the target compounds displayed excellent anthelmintic activities and the effects of compound 9a-b and 9g-h were much better than albendazole. This work provided a preliminary basis for developing novel antibacterial and anthelmintic agents. The further study on optimizing activities and mechanism-of-action is under investigation.