Park Joon Seok, Yu Kyung A, Kang Tae Hee, Kim Sunghoon, Suh Young-Ger
College of Pharmacy, Seoul National University, San 56-1 Shinrim-Dong, Kwanak-Gu, Seoul 151-742, Republic of Korea.
Bioorg Med Chem Lett. 2007 Jun 15;17(12):3486-90. doi: 10.1016/j.bmcl.2007.03.074. Epub 2007 Mar 27.
The in vitro and in vivo activities of a series of (2R,3R)-2-(2,4-difluorophenyl)-3-(substituted indazol-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol as potential antifungal agents are described. In particular, the analog 12j having 5-bromo substitution on the indazole ring exhibited significant antifungal activity against a variety of fungal cultures (Candida spp. and Aspergillus spp.). In addition, oral administration of 12j showed its excellent efficacy against Candida albicans in a murine infection model and the significantly improved survival rates of the infected mice.
描述了一系列(2R,3R)-2-(2,4-二氟苯基)-3-(取代吲唑-1-基)-1-(1H-1,2,4-三唑-1-基)丁-2-醇作为潜在抗真菌剂的体外和体内活性。特别地，在吲唑环上具有5-溴取代的类似物12j对多种真菌培养物（念珠菌属和曲霉属）表现出显著的抗真菌活性。此外，在小鼠感染模型中口服12j显示出其对白色念珠菌的优异疗效以及感染小鼠显著提高的存活率。
