摘要/Abstract

以朝格尔碱衍生物（5，12-二甲基-3，10-二苯基-双-1H-吡唑[b，f][4，5]-1，5-二氮杂双环[3.3.1]-2，6-辛二烯，1）为催化剂，以取代的α-溴代苯乙酮、芳香醛、丙二腈和硫脲为原料四组分一锅法合成了一系列噻唑并[3，2-a]嘧啶衍生物.通过¹H NMR和化学实验探讨了该反应的机理.体外药理活性实验结果表明，多个产物对人肝癌细胞（HepG2）、人非小细胞肺癌细胞（247）和人非小细胞肺癌细胞（A549）中的一个或多个细胞株具有较高抑制活性，七个产物对耐甲氧西林金黄色葡萄球菌具有抑菌活性.这些结果表明该类化合物在新药开发中具有巨大潜力.
关键词: Tröger碱衍生物, 催化, 噻唑并[3,2-a]嘧啶衍生物, 抗肿瘤, 抑菌
A series of thiazolo[3,2-a]pyrimidine derivatives were synthesized from the reaction of α-bromoacetophenone, aromatic aldehyde, malononitrile and thiourea which was catalyzed by Tröger's base derivative 5,12-dimethyl-3,10-diphenyl- bis-1H-pyrazol[b,f] [4,5]-1,5- diazadicyclo[3.3.1]-2,6-octadiene (1). The reaction mechanism was discussed by the ¹H NMR analysis and chemical experiments. The pharmacological activity results of the products indicated that most of products showed high inhibitory on one or more cancer cells in human hepatocarcinoma cell (HepG2), human non-small cell lung cancer cell (247) and human non-small cell lung cancer cell (A549) in vitro. And seven products have antibacterial activity against the methicillin-resistant Staphylococcus aureus. These results showed the great potential of these compounds in drug development.
Key words: Tröger's base derivative, catalysis, thiazolo[3,2-a]pyrimidine derivative, anti-tumor, anti-bacterial


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