Porretta G C, Cerreto F, Fioravanti R, Scalzo M, Fischetti M, Riccardi F, Capezzone de Joannon A, de Feo G, Mazzanti G, Tolu L
Istituto di Chimica Farmaceutica e Tossicologia, Facoltà di Farmacia, Università La Sapienza, Roma, Italy.
Farmaco Sci. 1988 Jan;43(1):15-28.
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.
报道了新型1,4 - 二芳基咪唑的合成、抗真菌及药理活性。与抗真菌抗生素硝吡咯菌素相比的抗菌数据指出，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。一些化合物对念珠菌属菌株表现出选择性活性。相反，药理数据未显示出任何显著的抗炎活性。所测试的化合物是通过使适当的苯甲酰苯胺与硫氰酸钾在酸性介质中反应制得1,4 - 二芳基 - 2 - 巯基咪唑，然后用硝酸处理将其转化为目标化合物。
