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2012 , Vol. 32 >Issue 01: 88 - 94

DOI: https://doi.org/10.6023/cjoc1107161

研究论文

新型吡啶-2-酮类衍生物的合成及生物活性

  • 曾永明 ,
  • 沈松伟 ,
  • 刘方明
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  • a 新疆大学化学化工学院 乌鲁木齐 830046;
    b 杭州师范大学材料与化学化工学院 杭州 310036

收稿日期: 2011-07-16

  修回日期: 2011-07-30

  网络出版日期: 2011-09-27

基金资助

国家自然科学基金(Nos. 29702007, 20162004)资助项目.

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Synthesis and Biological Activity of New 5-Heteroaryl-2-pyridone Derivatives

  • ZENG Yong-Ming ,
  • SHEN Song-Wei ,
  • LIU Fang-Ming
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  • a College of Chemistry and Chemical Engineering, Xinjiang University, Urumqi 830046;
    b College of Materials and Chemical Engineering, Hangzhou Normal University, Hangzhou 310036

Received date: 2011-07-16

  Revised date: 2011-07-30

  Online published: 2011-09-27

Supported by

Project supported by the National Natural Science Foundation of China (Nos. 29702007, 20162004).

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摘要

以3-氰基-5-乙酰基-6-甲基吡啶-2-酮(1a～1b)为原料, 通过多步反应, 合成了18 种未见报道的含有均三唑并[3,4-b][1,3,4]噻二嗪或1,3,4-噁二唑啉的两类新型吡啶酮类化合物4a～4h, 7a～7j, 其结构经1H NMR, IR 和MS 及元素分析确证. 利用单晶X 射线衍射法测定了化合物4a 的晶体结构. 初步生测表明, 部分化合物表现出不同的抗菌活性.

关键词： 均三唑并[3,4-b][1,3,4]噻二嗪; 1,3,4-噁二唑啉; 晶体结构; 抗菌活性

本文引用格式

曾永明 , 沈松伟 , 刘方明 . 新型吡啶-2-酮类衍生物的合成及生物活性[J]. 有机化学, 2012 , 32(01) : 88 -94 . DOI: 10.6023/cjoc1107161

Abstract

Eighteen title pyridone compounds containing the 1,3,4-oxadiazoline or 1,3,4-thiadiazine group were synthesized by the multi-step reaction using 5-acetyl-3-cyano-2-methyl-2-pyridone as stating materials. Structures of new compounds were characterized by 1H NMR, IR, MS techniques and elemental analysis. Compound 4a was further studied by single crystal X-ray diffraction analysis. The results of antibacterial activity experiment indicated that all compounds were all resistant to three different bacterias with various degrees.

Key words： 1,3,4-oxadiazoline; s-triazolo[3,4-b][1,3,4]thiadiazine; crystal structure; biological activity

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