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以2-(2-噻唑基)-3-乙酯基-4-甲基-1H-2,5-二氢-1,5-苯并二氮杂?(A)为模型化合物,设计合成了3个系列30种1H-2,5-二氢-1,5-苯并二氮杂?类衍生物2~6,其结构通过核磁共振波谱、红外光谱、质谱和元素分析确证.采用常规滤纸片扩散法测试了其对真菌(新生隐球菌标准株、临床株、白色念珠菌标准株)和细菌(大肠杆菌标准株和金黄色葡萄球菌标准株)的抑菌活性.研究结果表明,大多数化合物对所测试的菌种都表现出很好的抑制作用,且抑真菌能力大于抑细菌能力;通过对活性较高的化合物2-(2-噻唑基)-3-乙酯基-4-乙基-8-甲基-1H-2,5-二氢-1,5-苯并二氮杂?(4b)和2-(2-噻唑基)-3-乙酯基-4-乙基-8-氟-1H-2,5-二氢-1,5-苯并二氮杂?(4c)的最小抑菌浓度(MIC)和最小杀菌浓度(MFC)测试,发现其对白色念珠菌的MIC和MFC都远低于标准药物氟康唑.进一步构效关系研究表明C-2位的2-噻唑基,C-4位的CH_3、CH_2CH_3和C-8位的CH_3都是该类化合物抑菌的必需基团.
A 2-thiazolyl-3-carbomethoxy-4-methyl-1H-2,5-dihydro-1,5-benzodiazepine (A) Three series of 30 kinds of 1H-2,5-dihydro-1,5-benzodiazepine derivatives 2 ~ 6 whose structures were confirmed by 1H NMR, IR, MS and elemental analysis.Using conventional filter paper The antibacterial activity against fungi (Cryptococcus neoformans, clinical strains and Candida albicans) and bacteria (Escherichia coli and Staphylococcus aureus) were tested by diffusion-diffusion method.The results showed that most of the bacteria The compounds showed good inhibitory effect on the tested strains, and the ability of inhibiting fungi was greater than that of inhibiting bacteria. The higher activity of 2- (2-thiazolyl) -3-ethyl ester-4-B Dihydro-1,5-benzodiazepine (4b) and 2- (2-thiazolyl) -3-carbethoxy-4-ethyl- The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MFC) test of 8-fluoro-1H-2,5-dihydro-1,5-benzodiazepine (4c) MIC and MFC are far lower than the standard drug fluconazole further structure-activity relationship studies have shown that C-2 position 2-thiazolyl, C-4 position CH_3, CH_2CH_3 and C- 8-bit CH_3 is an essential group of antibacterial compounds of this group.