中华医学超声杂志

应用化学 ›› 2010, Vol. 27 ›› Issue (06): 651-657.DOI: 10.3724/SP.J.1095.2010.90513

• 研究论文 • 上一篇    下一篇

含脱羧脱氢松香基的1,2,4-三唑并[3,4-b]-1,3,4-噻二唑衍生物的合成、表征及抑菌活性

苏桂发1*,周艺明1,覃江克1,邓业成2,张明2,王忠长1,宗玺1   

  1. (1.广西师范大学化学化工学院,药用资源化学与药物分子工程教育部重点实验室 桂林 541004;
    2.广西师范大学生命科学学院 桂林)
  • 收稿日期:2009-07-30 修回日期:2009-12-30 出版日期:2010-06-10 发布日期:2010-06-10
  • 通讯作者: 苏桂发,男,博士,教授; E-mail:edward_su75@163.com; 研究方向：精细有机合成
  • 基金资助:
    专项基金(2004219)广西科技开发计划应用基础研究专项(桂科基0731054)资助项目

Synthesis, Characterization and Antibacterial Activity of 3-Substituted-6-(4′-decarboxydehydroabietyl)-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole Derivatives

SU Gui-Fa1*, ZHOU Yi-Ming1, QIN Jiang-Ke1, DENG Ye-Cheng2, ZHANG Ming2, WANG Zhong-Chang1, ZONG Xi1   

  1. (1.Key Laboratory for the Chemistry and Molecular Engineering of Medicial Resources of State Education
    Ministry,College of Chemistry & Chemical Engineering,Guangxi Normal University,Guilin 541004;
    2.College of Life Science,Guangxi Normal University,Guilin 541004)
  • Received:2009-07-30 Revised:2009-12-30 Published:2010-06-10 Online:2010-06-10
  • Contact: Guifa SU

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摘要：

用POCl3为催化剂和脱水剂,3-取代-4-氨基-5-巯基-1,2,4-三唑4和10分别与脱氢松香酸1反应制得14种未见文献报道的3-取代-6-(4′-脱羧脱氢松香基)-1,2,4-三唑并[3,4-b-]-1,3,4-噻二唑衍生物]5a~5e和11a~11i;所有化合物的结构均经IR、1H NMR、13C NMR 和MS测试技术分析确认。 抑菌活性测试表明,目标化合物对白色念珠菌(C.Albicans)、大肠杆菌(E.Coli)、藤黄微球菌(M.Luteus)和痢疾志贺杆菌(S.Dysenteriae)均有一定的抑制作用。

关键词: 脱氢松香酸, 三唑并[3,4-b]噻二唑, 抑菌活性

Abstract:

Fourteen new 3-substituted-6-(4′-decarboxydehydroabietyl)-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles 5a~5e and 11a~11i were obtained from the reaction of 3-substituted-4-amino-5-mercapto-1,2,4-triazoles 4 and 10 with dehydroabietic acid ]1 in the presence of phosphorus oxychloride, respectively. All target compounds were characterized by IR, 1H NMR, 13C NMR and MS. The preliminary antibacterial activity assay showed that title compounds 5 and 11 exhibited a fungicidal activity against C.Albicans, E.coli., M.Luteus and S.Dysenteriae.

Key words: dehydroabietic acid, triazolo[3,4-b]-thiadiazole, antibacterial activity

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