一些乙烯基取代的2-硝基咪唑的合成与生物活性

Synthesis and biological activity of some vinyl-substituted 2-nitroimidazoles.

作者信息

Cavalleri B, Volpe G, Arioli V

出版信息

J Med Chem. 1977 May;20(5):656-60. doi: 10.1021/jm00215a007.

DOI:10.1021/jm00215a007

PMID:16132

Abstract

In previous studies 1-methyl-2-nitro-1H-imidazole-5-carboxaldehyde and 1-methyl-2-nitro-5-vinyl-1H-imidazole were found to posses interesting antimicrobial activities. We have now prepared some 2-nitro-1H-imidazoles in which the 5-vinyl chain bears selected functional groups (CHO, COCH3, NO2) as well as nitrogen-condensation derivatives of the carbonyl functions. Furthermore, 5-methyl-2-nitro-1-vinyl-1H-imidazole has been synthesized. All the compounds, and some intermediates, have been assayed for antimicrobial activity. Several of them exhibited significant antibacterial and antitrichomonal activity in mice.

摘要

在先前的研究中，发现1-甲基-2-硝基-1H-咪唑-5-甲醛和1-甲基-2-硝基-5-乙烯基-1H-咪唑具有有趣的抗菌活性。我们现已制备了一些2-硝基-1H-咪唑，其中5-乙烯基链带有选定的官能团（CHO、COCH3、NO2）以及羰基官能团的氮缩合衍生物。此外，还合成了5-甲基-2-硝基-1-乙烯基-1H-咪唑。所有这些化合物以及一些中间体都已进行抗菌活性测定。其中几种在小鼠中表现出显著的抗菌和抗滴虫活性。

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