新型吡啶-2-酮类衍生物的合成及生物活性

Synthesis and Biological Activity of New 5-Heteroaryl-2-pyridone Derivatives

以3-氰基-5-乙酰基-6-甲基吡啶-2-酮(1a～1b)为原料,通过多步反应,合成了18种未见报道的含有均三唑并[3,4-b][1,3,4]噻二嗪或1,3,4-噁二唑啉的两类新型吡啶酮类化合物4a～4h,7a～7j,其结构经1H NMR,IR和MS及元素分析确证.利用单晶X射线衍射法测定了化合物4a的晶体结构.初步生测表明,部分化合物表现出不同的抗菌活性.

Eighteen title pyridone compounds containing the 1,3,4-oxadiazoline or 1,3,4-thiadiazine group were synthesized by the multi-step reaction using 5-acetyl-3-cyano-2-methyl-2-pyridone as stating materials.Structures of new compounds were characterized by 1H NMR,IR,MS techniques and elemental analysis.Compound 4a was further studied by single crystal X-ray diffraction analysis.The results of antibacterial activity experiment indicated that all compounds were all resistant to three different bacterias with various degrees.