含三唑席夫碱双枝吡啶类衍生物的微波合成及其抗菌活性研究

在微波辐射条件下,由2,4-吡啶二甲酸出发,依次经过酯化、肼解、成环、消除,高产率的合成了10个未见文献报道的新型吡啶类席夫碱类化合物.通过微波法和常规法的对比发现,使用微波法后,产率从49%—70%提高到77%—90%,反应时间从360分钟缩短到10—15分钟.所有目标物的结构均经IR,~1H NMR,ESI-MS及元素分析所确证.部分化合物测试了其对杆金黄色葡萄球菌、大肠杆菌、枯草芽孢菌的抗菌活性.实验结果表明,化合物6b,6c,6d对金黄色葡萄球菌、大肠杆菌、枯草芽孢菌表现出较好的抑菌活性,同时从构效关系看,卤素原子的引入有助于提高化合物的抑菌活性.邻位取代基比对位取代基的抑菌活性好.该结果对抑菌先导化合物的设计具有一定的参考价值.

Microwave-prompted synthesis and bioactivity of novel substituted bis-triazole Schiff bases containing pyridine rings

Ten novel pyridine Schiff bases were efficiently synthesized through esterification, hydrazine, ring formation, and elimination reaction by using 2,4-pyridinedicarboxylic acid via a method employing microwave irradiation. The structures were characterized by ₁H NMR, ESI-MS spectra, IR and elemental analysis. Antibacterial activity against Escherichia coli, Bacillus subtilis and Staphyloccocus aureus was tested with the view of providing lead compounds for the screening of new drugs