新型含卤噻唑类酰腙化合物的合成及其与小牛胸腺DNA的相互作用

以2-氨基噻唑-4-甲酸乙酯和水合肼为原料，制得2-氨基噻唑-4-甲酰肼(2)； 2与卤代(F, Cl, Br)对苯甲醛反应，合成了3种新型的含卤噻唑类酰腙化合物［C₁₁H₉N₄OSF(3a), C₁₁H₉N₄OSCl(3b)和C₁₁H₉N₄OSBr(3c)］，其结构和性能经元素分析，XRD和TG-DTG表征。结果表明：3a和3c属于三斜晶系，Pī空间群；3b属于单斜晶系，P2(1)/c空间群。3a~3c的热稳定性均较好，最大热分解过程的表观活化能均大于100 kJ·mol^-1。采用UV-Vis研究了3a~3c与小牛胸腺DNA(CT-DNA)的相互作用。结果表明：3a~3c与CT-DNA均以插入方式相互作用。

Synthesis of Novel Thiazole Acylhydrazone Compounds Containing Halogen Atoms and Their Interaction with CT-DNA

2-Aminothiazole-4-formylhydrazine(2)was obtained by the reaction of 2-aminothiazole-4-methylformate with hydrazine hydrate.Three novel thiazole acylhydrazone compounds containing halogen atomsC11H9N4OSF(3a), C11H9N4OSCl(3b) and C11H9N4OSBr(3c)] were synthesized by the reaction of 2 with halogenated benzaldehydes(F, Cl, Br).The structures and properties were characterized by elemental analysis, XRD and TG-DTG.The results showed that 3a and 3c belong to triclinic, space group Pī, and 3b belongs to monoclinic, space group P2(1)/c.3a~3c exhibited good thermal stabilities with apparent activation energies above 100 kJ·mol-1 during the maximum thermal decomposition processes.The interaction of 3a~3c with CT-DNA were investigated by UV-Vis.The results indicated that 3a~3c interact with CT-DNA by the mode of insert.