新型芳醛并苯甲酰腙类化合物的合成及其抗结核活性  

Synthesis and Antituberculous Activities of Novel Aromatic Aldehyde Benzoyl Hydrazone Derivatives

作　　者：卢久富[1] 白跃飞 周鹏 

机构地区：[1]陕西理工学院化学学院,陕西汉中723001 [2]东北制药集团股份有限公司,辽宁沈阳110026 [3]东北制药(沈阳)施德药业有限公司,辽宁沈阳110026

出　　处：《合成化学》2015年第1期31-35,共5页Chinese Journal of Synthetic Chemistry

基　　金：陕西省教育厅科学研究项目(12JK0637)

摘　　要：以2-氨基-5-取代苯甲酸甲酯或2-氨基-5-哌啶基苯磺酰胺为起始原料,经酰化、胺基化、肼解和缩合反应合成了10个新型的芳醛并苯甲酰腙类化合物(8a^8i或Ⅳ),其结构经1H NMR和ESI-MS表征。初步研究了8a^8i和Ⅳ的抗结核活性。结果表明:8c对结核分枝杆菌H37Rv和草分枝杆菌1180的MIC分别为9μg·m L-1和11μg·m L-1,与阳性对照药异烟肼(7μg·m L-1和8μg·m L-1)和利福平(8μg·m L-1和10μg·m L-1)的抑制活性相当。Ten novel aromatic aldehyde benzoyl hydrazone derivatives（ 8a ～ 8i or Ⅳ） were synthesized by acylation reaction of 2-amido-5-substituted methyl benzoate（ or 2-amido-5-piperidyl-benzene sulfonamide） with arylacylchloride,followed by amination,hydrazinolysis and condensation with arylaldehyde. The structures were characterized by^1 H NMR and ESI-MS. The antituberculous activities of 8a ～ 8i and Ⅳ were investigated. The results showed that MIC of 8c were 9 μg · m L^-1and11 μg·m L^-1on M. tuberculosis H37 Rv and M. phlei 1180 cells. Inhibitory activity of 8c was similar to isoniazid and rifampicin.

关 键 词：芳醛并苯甲酰腙 药物合成 抗结核活性 

分 类 号：O521.3[理学—高压高温物理] R914.5[理学—物理]