3-吡啶甲醛-4-噁唑甲酰腙的合成及生物活性研究  

Research on Synthesis and Biological Activities of 3-Pyridylformaldehyde-4-Oxazolylhydrazone

作　　者：宋长磊 张芳芳 张帅 段玉娥 杜庆波 SONG Changlei;ZHANG Fangfang;ZHANG Shuai;DUAN Yu’e;DU Qingbo(Department of Pharmacy,North Anhui Health Vocational College,Suzhou 234000,China;Key Laboratory of Medicinal Resource Chemistry and Natural Pharmacology of Suzhou,North Anhui Health Vocational College,Suzhou 234000,China;Hefei BOE Hospital,Hefei 230000,China;Suzhou Yifan Pharmaceutical Co.,Ltd,Suzhou 234000,China)

机构地区：[1]皖北卫生职业学院药学系,安徽宿州234000 [2]皖北卫生职业学院宿州市药用资源化学与天然药物学重点实验室,安徽宿州234000 [3]合肥京东方医院,安徽合肥230000 [4]宿州亿帆药业有限公司,安徽宿州234000

出　　处：《新乡学院学报》2025年第3期23-29,共7页Journal of Xinxiang University

基　　金：安徽省教育厅2021年高校拔尖人才项目(gxbjZD2021114);安徽省教育厅质量工程项目(2021ixtd300)。

摘　　要：以4-噁唑甲酸乙酯和水合肼为原料合成4-噁唑甲酰肼,再与3-吡啶甲醛反应合成了新型噁唑类酰腙化合物(3-吡啶甲醛-4-噁唑甲酰腙),得到了该化合物的单晶,测定了其熔点,元素分析表明其分子式为C_(10)H_(8)N_(4)O_(2)。借助X射线单晶衍射对单晶结构进行表征,结果表明该化合物属于单斜晶系,空间群为Pn。通过热重实验测定其热稳定性,并计算了表观活化能(Ea),结果显示该化合物热稳定性较高。利用紫外光谱和黏度实验研究了合成的酰腙化合物与小牛胸腺蛋白(CT-DNA)的相互作用,发现其与CT-DNA相互作用的模式为插入模式;利用荧光光谱探究了其和牛血清蛋白(BSA)的相互作用,结果表明它与BSA的相互作用是静态猝灭的过程:说明合成的噁唑类酰腙化合物具有较好的生物活性。4-Oxazolecarboxylic acid hydrazide was synthesized by the condensation reaction of 4-Oxazolecarboxylic acid ethyl ester and hydrazine hydrate,which was then reacted with 3-Pyridinecarboxylic acid to get a novel oxazole acylhydrazone compound(3-Pyridylformaldehyde-4-Oxazolylhydrazone).The single crystal of the compound was obtained,and its melting point was determined.Elemental analysis showed that its molecular formula was C_(10)H_(8)N_(4)O_(2).The single crystal structure was characterized by X-ray single crystal diffraction,and the results showed that the compound belongs to the monoclinic crystal system,with space groups Pn,respectively.The thermal stability of the compound was determined through thermogravimetric experiments,and the apparent activation energy(Ea)was calculated.The results showed that the compound had high thermal stability.The interaction between the synthesized acylhydrazone compound and calf thymus protein(CT-DNA)and bovine serum albumin(BSA)was studied using UV spectroscopy and viscosity experiments,and it was found that the interaction mode with CT-DNA was insertion mode;The interaction between it and bovine serum albumin(BSA)was investigated using fluorescence spectroscopy,and the results showed that there was a static quenching process between it and BSA,indicating that the synthesized oxazole acylhydrazone compounds have good biological activity.

关 键 词：噁唑类酰腙化合物 晶体结构 热稳定性 生物活性 

分 类 号：O641.4[理学—物理化学]