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2-(3-吡啶)-5-{[(5-芳基-1,3,4-二唑-2-基)亚甲基]硫代}-1,3,4-二唑的合成及抗菌活性
引用本文:胡国强,许秋菊,刘宝,张忠泉,陈百泉,许启泰,黄文龙,张惠斌,黄胜堂. 2-(3-吡啶)-5-{[(5-芳基-1,3,4-二唑-2-基)亚甲基]硫代}-1,3,4-二唑的合成及抗菌活性[J]. 药学学报, 2004, 39(4): 263-265
作者姓名:胡国强  许秋菊  刘宝  张忠泉  陈百泉  许启泰  黄文龙  张惠斌  黄胜堂
作者单位:[1]河南大学药学院,河南开封475004 [2]中国药科大学新药中心,江苏南京210009
摘    要:目的研究多杂环化合物的合成方法和抗菌活性。方法用[(5-吡啶-3-基-1,3,4-二唑-2-基)硫代]乙酸与相应的芳酰肼缩合,得到相应的目标化合物。用试管稀释法,研究目标化合物的体外抑菌活性。结果合成了16个新化合物,其结构经MS,IR,1HNMR和元素分析确证。其中多数化合物在体外表现出较好的抑菌活性。结论 含吡啶的双二唑杂环化合物有可能成为新型结构的抗菌药物。

关 键 词:杂环化合物  二唑  合成  抗菌活性
收稿时间:2003-05-26

Synthesis and antibacterial activity of 2-(3-pyridyl)-5-([(5-aryl-1,3,4-oxadiazol-2-yl) methylene]thio)-1,3,4-oxadiazoles]
HU Guo-qiang,XU Qiu-ju,LIU Bao,ZHANG Zhong-quan,CHEN Bai-quan,XU Qi-tai,HUANG Wen-long,ZHANG Hui-bin,HUANG Sheng-tang. Synthesis and antibacterial activity of 2-(3-pyridyl)-5-([(5-aryl-1,3,4-oxadiazol-2-yl) methylene]thio)-1,3,4-oxadiazoles][J]. Acta pharmaceutica Sinica, 2004, 39(4): 263-265
Authors:HU Guo-qiang  XU Qiu-ju  LIU Bao  ZHANG Zhong-quan  CHEN Bai-quan  XU Qi-tai  HUANG Wen-long  ZHANG Hui-bin  HUANG Sheng-tang
Affiliation:Medical College of Henan University, Kaifeng 475004, China. hgqxy@sina.com.cn
Abstract:AIM: Studies on synthesis and antibacterial activity of new heterocycles. METHODS: The cyclocondensation of [(3-pyridyl)-1,3,4-oxadiazol-2-yl] thio acetic acid with various aroyl hydrazines in the presence of POCl3 and xylene gave the corresponding titled compounds, and the in vitro antibacterial activity was primarily evaluated by the method of cupplate diffusion solution. RESULTS: Sixteen novel titled compounds were synthesized, their structures were confirmed by IR, 1HNMR, MS and elemental analysis. Biological screening results demonstrated that most of the compounds prepared displayed potential antibacterial activity. CONCLUSION: Oxadiazoles incorporting pyridyl oxadiazole ring may be usefully antibacterial candidate drugs.
Keywords:oxadiazole  synthesis  antimicrobial activity  heterocycle
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