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新型1,2-双(1,3,4-恶二唑-2-基)乙烷和1,2-双(4-氨基-1,2,4-三唑-3-基)乙烷系列的合成与抗菌研究

Synthesis and antibacterial studies of a new series of 1,2-bis(1,3, 4-oxadiazol-2-yl)ethanes and 1,2-bis(4-amino-1,2, 4-triazol-3-yl)ethanes.

作者信息

Holla B S, Gonsalves R, Shenoy S

机构信息

Department of Post Graduate Studies and Research in Chemistry, Mangalore University, Mangalagangothri, India.

出版信息

Eur J Med Chem. 2000 Feb;35(2):267-71. doi: 10.1016/s0223-5234(00)00154-9.

DOI:10.1016/s0223-5234(00)00154-9
PMID:10758288
Abstract

The acylhydrazones 3, obtained by the treatment of succinic acid dihydrazide 2 with furfural, nitrofurfuraldehydediacetate and substituted arylfurfurals, on oxidative cyclization with bromine in acetic acid yielded 1,2-bis(1,3,4-oxadiazol-2-yl)ethanes 4 which are further converted into 1,2-bis(4-amino-1,2,4-triazol-3-yl)ethanes 5 with hydrazine hydrate. The newly synthesised compounds are characterised by analytical, IR, NMR and mass spectral data. Most of the newly synthesised compounds have been found to be active against both Gram positive and Gram negative bacteria at less than 6 microg/mL concentration.

摘要

通过用糠醛、硝基糠醛二乙酸酯和取代芳基糠醛处理琥珀酸二酰肼2得到酰腙3,其在乙酸中用溴进行氧化环化反应生成1,2-双(1,3,4-恶二唑-2-基)乙烷4,4再与水合肼反应转化为1,2-双(4-氨基-1,2,4-三唑-3-基)乙烷5。新合成的化合物通过分析、红外、核磁共振和质谱数据进行表征。已发现大多数新合成的化合物在浓度低于6微克/毫升时对革兰氏阳性菌和革兰氏阴性菌均有活性。

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