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一些含有异构吡啶基的新型2,5-二取代1,3,4-噻二唑作为强效抗菌剂的合成。

Synthesis of some new 2,5-disubstituted 1,3,4-thiadiazoles containing isomeric pyridyl as potent antimicrobial agents.

作者信息

Zamani Khosrow, Faghihi Khalil, Mehranjani Malek S

机构信息

Department of Chemistry, Arak University, Arak, Iran.

出版信息

Pol J Pharmacol. 2003 Nov-Dec;55(6):1111-7.

Abstract

Several new 2,5-disubstituted derivatives of 1,3,4-thiadiazoles containing isomeric pyridyl were obtained from cyclization of corresponding thiosemicarbazides under acidic conditions. The newly synthesized compounds were characterized using different methods of spectroscopy such as IR, 1H-NMR, 13C-NMR, MS and elemental analysis. The minimal inhibitory concentration (MIC) results of screening of some of the synthesized compounds were also reported. Most of the synthesized compounds have been found to be active against both Gram-positive and Gram-negative bacteria at less than 3.6 mg/ml. The compound (10b) is most active against all seventeen used gram-positive and gram-negative bacteria.

摘要

通过相应的氨基硫脲在酸性条件下环化反应,得到了几种含异构吡啶基的新型1,3,4 - 噻二唑2,5 - 二取代衍生物。采用红外光谱(IR)、氢核磁共振谱(1H - NMR)、碳核磁共振谱(13C - NMR)、质谱(MS)和元素分析等不同光谱方法对新合成的化合物进行了表征。还报道了部分合成化合物的最低抑菌浓度(MIC)筛选结果。已发现大多数合成化合物对革兰氏阳性菌和革兰氏阴性菌均有活性,浓度低于3.6 mg/ml。化合物(10b)对所有使用的17种革兰氏阳性菌和革兰氏阴性菌活性最强。

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