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二取代和三取代咪唑的合成及生物学筛选

Synthesis and biological screening of di- and trisubstituted imidazoles.

作者信息

Husain Asif, Drabu Sushma, Kumar Nitin

机构信息

Faculty of Pharmacy, Jamia Hamdard University, Department of Pharmaceutical Chemistry, Hamdard Nagar, New Delhi-110062, India.

出版信息

Acta Pol Pharm. 2009 May-Jun;66(3):243-8.

PMID:19645324
Abstract

Disubstituted imidazoles were prepared by reacting appropriate phenylglyoxal with different aryl aldehydes in the presence of ammonium acetate. Trisubstituted imidazoles were prepared by reacting disubstituted imidazoles with chlorobenzene in the presence of catalytic amount of triethylamine (TEA). The synthesized compounds were characterized on the basis of IR, 1H-NMR and mass spectral data and elemental analysis results. They were tested for their antiinflammatory and antimicrobial actions. Two compounds showed good antiinflammatory activity in carrageenan induced rat paw edema test with very low ulcerogenic activity. Fair number of compounds were found to have significant antimicrobial activity especially against fungal species.

摘要

通过在乙酸铵存在下使适当的苯乙二醛与不同的芳醛反应制备二取代咪唑。通过在催化量的三乙胺(TEA)存在下使二取代咪唑与氯苯反应制备三取代咪唑。根据红外光谱、1H-NMR、质谱数据和元素分析结果对合成的化合物进行表征。对它们的抗炎和抗菌作用进行了测试。两种化合物在角叉菜胶诱导的大鼠足肿胀试验中显示出良好的抗炎活性,且致溃疡活性非常低。发现相当数量的化合物具有显著的抗菌活性,尤其是对真菌种类。

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