高等学校化学学报

高等学校化学学报 ›› 1991, Vol. 12 ›› Issue (10): 1344.

• 论文 • 上一篇    下一篇

稠杂环化合物的研究(Ⅳ)--5-醛胺基-1-芳基-1,2,3-连三唑[2,3-d]嘧啶-4-酮类衍生物的合成及抗菌性能

张自义1, 刘莹1, 杨世琰2, 陈茂齐2   

  1. 1. 兰州大学化学系, 兰州, 730000;
    2. 中国科学院兰州化学物理研究所
  • 收稿日期:1990-07-08 出版日期:1991-10-24 发布日期:1991-10-24
  • 通讯作者: 张自义

Studies on Condensed Heterocyclic Compounds (Ⅳ)--Synthesis and Antibacterial Activity of 5-Formylamino-l-Aryl-1,2,3-Triazolo(2,3-d)Pyrimidin-4 one and Their Related Derivatives

Zhang Zi-yi1, Liu Ying1, Yang Shi-yan2, Chen Mao-qi2   

  1. 1. Department of Chemistry, Lanzhou University, Lanzhou, 730000;
    2. Lanzhou Institute of Chemical Physics, Academia Sinica, Lanzhou
  • Received:1990-07-08 Online:1991-10-24 Published:1991-10-24

PDF (PC)

被引次数

8

摘要： 我们已报道了1-芳基-4-乙氧羰基-5-氨基-1,2,3-连三唑类衍生物(1)的合成及抗菌活性,为研究药物构效关系,我们利用1的酰肼3同甲酸反应,制得了尚未报道的5-醛胺基-1-芳基-1,2,3-连三唑[2,3-d]嘧啶-4-酮(4a-c)及5-氨基-6-羟基-7H-1-(间硝基)苯基-1,2,3-连三唑[2,3-d]嘧啶-4-酮(5d).并观察了它们对枯草杆菌,金黄色葡萄球菌等繁殖的抑制作用。

关键词: 连三唑并嘧啶酮, 合成, 抗菌活性

Abstract: 5-Formylamino-1-aryl-1,2,3-triazolo(2, 3-d)pyrimidin-4-one (4a,b,c) and 5-amino-6-hydroxyl-7H-1-(m-nitrophenyl)-1,2,3-triazolo(2,3-d)pyrimidin-4-one (5d) have been synthesised fromthe reaction of 1-aryl-4-carbonhydrazide-5-amino-1, 2, 3-triazoles 3a,b,c,dprepared by hydrazinolysis of either 1-aryl-4-ethoxycarbonyl-5-amino-1, 2, 3-triazoles 1a,b,c,dor their benzoylamino derivatives (2a,d), with an excess of formic acid under the fluxing condition. The structures of all heterocyclic compounds were confirmed by elemental analysis, IR,1HNMR, MS, and the inhibiting effects on B. Substilis; E. coli; E. aerogenes;S. aureus were also screened.

Key words: Triazolopyrimidinone, Synthesis, Antibacterial activity

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