Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols
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新型1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-取代的苄氨基-2-丙醇的设计、合成和生物学评价
DOI：
10.1016/j.bmcl.2009.01.048
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发表时间：
2009-03-15
影响因子：
2.7
通讯作者：
Wu, Qiuye
中科院分区：
文献类型：
--
作者：
Chai, Xiaoyun;Zhang, Jun;Wu, Qiuye
基于与细胞色素P450 14 α-去甲基酶（CYP 51）活性位点的计算机对接结果，设计、合成了一系列1-（1H-1，2，4-三唑-1-基）-2-（2，4-二氟苯基）-3-取代苄氨基-2-丙醇类氟康唑类似物，并对其抗真菌活性进行了评价。对8种人体病原真菌的初步体外抗真菌活性测试结果表明，所有标题化合物均表现出良好的广谱抗真菌活性。(C)2009爱思唯尔有限公司保留所有权利。
Based on the results of computational docking to the active site of the cytochrome P450 14 alpha-demethylase (CYP51), a series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols as analogs of fluconazole were designed, synthesized, and evaluated as antifungal agents. Results of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that all the title compounds exhibited excellent activities with broad spectrum. (C) 2009 Elsevier Ltd. All rights reserved.