新环6-甲基咪唑[1,2-d]并-1,2,3,4-噻三唑-5-羧酸衍生物的合成
Synthesis of Neoring 6-Methylimidazo[1,2-d][1,2,3,4]thiatriazole-5-carboxylic Acid Derivatives

作者: 钞智锋 , 布 仁 * , 鲁 源 :内蒙古医科大学,呼和浩特;

关键词: 5-氨基-1234-噻三唑咪唑[12-d]并-1234-噻三唑生物活性5-Amino-1234-thiatriazole Imidazo[12-d][1234]thiatriazole Biological Activity

摘要:

目的:为了寻找抑制细胞分裂周期磷酸酯酶CDC25B抗肿瘤新药,设计和合成6-甲基-咪唑[1,2-d]-1,2,3,4-噻三唑-5-羧酸衍生物是有意义的。方法:5-氨基-1,2,3,4-噻三唑和溴代乙酰乙酸乙酯为原料,经过关环,肼解,缩合等反应合成目标化合物。结果:合成了5种新的化合物。结论:所得化合物,通过元素分析、IR1H NMR和质谱分析确定了其结构,并且化合物34aCDC25B的抑制率(%抑制率)分别为85.482.3,具有一定的生物活性。
Objective: In order to search the new anti-cancer drugs inhibiting with cell division cycle CDC25B phosphatase, designing and synthesizing 6-Methylimidazo[1,2-d][1,2,3,4]thiatriazole-5-carboxylic acid derivatives is meaningful. Methods: The objective compounds were synthesized by cyclization, hydrazinolysis, condensation in the basis of 5-amino-1,2,3,4-triazole and bromine ethyl acetoacetate. Result: The five new kinds of compounds were synthesized. Conclusion: The structures of the compounds were determined by elemental analysis, IR, 1H NMR and MS, furthermore, it was found that the inhibition rates (% inhibition) of the CDC25B were 85.4 and 82.3 by compounds 3 and 4a with a certain biological activity.

文章引用: 钞智锋 , 布 仁 , 鲁 源 (2013) 新环6-甲基咪唑[1,2-d]并-1,2,3,4-噻三唑-5-羧酸衍生物的合成。 药物化学, 1, 1-4. doi: 10.12677/HJMCE.2013.11001

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