抗真菌剂。III. 1H-咪唑-1-基-4-苯基-1H-吡咯-3-基甲烷的萘基和噻吩基衍生物
Antifungal agents. III. Naphthyl and thienyl derivatives of 1H-imidazol-1-yl-4-phenyl-1H-pyrrol-3-ylmethane.
作者信息
Massa S, Di Santo R, Costi R, Simonetti G, Retico A, Apuzzo G, Artico M
机构信息
Dipartimento di Studi Farmaceutici, Università di Roma, La Sapienza.
出版信息
Farmaco. 1993 Jun;48(6):725-36.
The in vitro antifungal activities of some naphthyl and thienyl derivatives of 1H-imidazol-1-yl-4-phenyl-1H-pyrrol-3-ylmethane against Candida albicans and Candida spp are reported. The title derivatives were prepared starting from proper arylstirylketones, which were reacted with tosylmethylisocyanide (Tos-MIC) to afford the related 4-phenyl-1H-pyrrol-3-yl aryl ketones. Reduction of ketones to the corresponding carbinols followed by treatment of the last compounds with 1,1'-carbonyldiimidazole (CDI) gave the title imidazoles. The related N-methylpyrrole derivatives are also described.
报道了1H-咪唑-1-基-4-苯基-1H-吡咯-3-基甲烷的一些萘基和噻吩基衍生物对白色念珠菌和念珠菌属的体外抗真菌活性。标题衍生物由适当的芳基苯乙烯基酮开始制备，芳基苯乙烯基酮与对甲苯磺酰甲基异腈（Tos-MIC）反应得到相关的4-苯基-1H-吡咯-3-基芳基酮。将酮还原为相应的甲醇，然后用1,1'-羰基二咪唑（CDI）处理这些化合物，得到标题咪唑。还描述了相关的N-甲基吡咯衍生物。
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