三唑类抗真菌药。IV。3-酰氨基-2-芳基-2-丁醇衍生物的合成与抗真菌活性
Triazole antifungals. IV. Synthesis and antifungal activities of 3-acylamino-2-aryl-2-butanol derivatives.
作者信息
Konosu T, Tajima Y, Takeda N, Miyaoka T, Kasahara M, Yasuda H, Oida S
机构信息
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
出版信息
Chem Pharm Bull (Tokyo). 1991 Oct;39(10):2581-9. doi: 10.1248/cpb.39.2581.
New triazole compounds were designed and synthesized as potential inhibitors of the fungal cytochrome P-450 14 alpha-demethylase. In testing for antifungal activity against a mouse systemic Candida albicans infection, (2R,3R)-3-acylamino-2-aryl-2-butanol derivatives III exhibited remarkably high efficacy after oral or parenteral administration. The structure-activity relationships of these amidoalcohols were evaluated.
设计并合成了新型三唑化合物，作为真菌细胞色素P-450 14α-脱甲基酶的潜在抑制剂。在针对小鼠全身性白色念珠菌感染的抗真菌活性测试中，(2R,3R)-3-酰氨基-2-芳基-2-丁醇衍生物III经口服或肠胃外给药后显示出极高的疗效。对这些酰胺醇的构效关系进行了评估。
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