Wu Q Y, Li K, Liu C M, Liu G X, Wang X Y
Department of Medicinal Chemistry, College of Pharmacy, Second Military Medical University, Shanghai.
Yao Xue Xue Bao. 1993;28(9):661-7.
Twenty nine 1-(2-[(4-substituted-phenyl) methoxy]-2-(substituted-phenyl) ethyl)-1H-azoles were synthesized for searching of more potent and less toxic antimycotic agents. Nine of the title compounds are first reported. Results of preliminary biological tests showed that most of the title compounds exhibited activity against the common pathogenic fungi such as Candida albicans, Microsporum bodin, Trichophyton gypsum, Epidermophyton floccosum, Trichophyton violaceum, Microsporum ferrugincum, Trichophyton rubrum and Microsporum gypsum. The antifungal activity of compound 14 was roughly comparable to clotrimazole and econazole against Candida albicans, but was more active against other test fungi than clotrimazole and econazole. Compounds 4, 5, 6, 12, 23 also have good antifungal activity, but are less active against Candida albicans.
为了寻找更有效且毒性更低的抗真菌药物，合成了29种1-(2-[(4-取代苯基)甲氧基]-2-(取代苯基)乙基)-1H-唑类化合物。其中9种标题化合物为首次报道。初步生物学测试结果表明，大多数标题化合物对常见致病真菌如白色念珠菌、博迪小孢子菌、石膏样毛癣菌、絮状表皮癣菌、紫色毛癣菌、铁锈色小孢子菌、红色毛癣菌和石膏样小孢子菌具有活性。化合物14对白色念珠菌的抗真菌活性与克霉唑和益康唑大致相当，但对其他受试真菌的活性比克霉唑和益康唑更强。化合物4、5、6、12、23也具有良好的抗真菌活性，但对白色念珠菌的活性较低。
