含有咪唑基团的化疗药物。2新型1,4-二芳基咪唑的合成及生物活性研究。

Il Farmaco; edizione scientifica Pub Date : 1988-01-01
G C Porretta, F Cerreto, R Fioravanti, M Scalzo, M Fischetti, F Riccardi, A Capezzone de Joannon, G de Feo, G Mazzanti, L Tolu
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引用次数: 0

摘要

报道了新型1,4-二芳基咪唑的合成、抗真菌活性和药理活性。与抗真菌抗生素吡咯硝唑的比较表明,1,4-二芳基-2-巯基咪唑衍生物无活性,所有1,4-二芳基咪唑均表现出较弱的抗真菌活性。一些化合物显示出对念珠菌菌株的选择性活性,而药理学数据没有显示任何显著的抗炎活性。在酸性介质中,适当的苯基苯胺与硫氰酸钾反应得到1,4-二芳基-2-巯基咪唑,再经硝酸处理转化为标题化合物。
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Chemotherapeutic agents with an imidazole moiety. II. Synthesis and biological activities of new 1,4-diarylimidazoles.

The synthesis, antifungal and pharmacological activities of new 1,4-diarylimidazoles are reported. Antimicrobial data in comparison with antifungal antibiotic pyrrolnitrin pointed out that the 1,4-diaryl-2-mercaptoimidazole derivatives were inactive and all 1,4-diarylimidazoles exhibited a weak antifungal activity. Some compounds showed a selective activity against strains of Candida sp. Instead pharmacological data did not evidence any significant antiinflammatory activity. The tested compounds were prepared by reacting appropriate phenacylanilines with potassium thiocyanate in acidic medium to afford 1,4-diaryl-2-mercapto imidazoles which were then transformed into title compounds by treatment with nitric acid.

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