Imidazole analogues of fluoxetine, a novel class of anti-Candida agents.
Imidazole analogues of fluoxetine, a novel class of anti-Candida agents.
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DOI：
10.1021/jm049856v
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发表时间：
2004-07
影响因子：
7.3
通讯作者：
R. Silvestri;M. Artico;G. La Regina;Alessandra Di Pasquali;G. De Martino;F. D. D'Auria;L. Nencioni;A. Palamara
中科院分区：
文献类型：
--
作者：
R. Silvestri;M. Artico;G. La Regina;Alessandra Di Pasquali;G. De Martino;F. D. D'Auria;L. Nencioni;A. Palamara
通过用咪唑环取代氨基丙烷链的甲氨基末端，得到氟西汀的咪唑类似物。新设计的咪唑类化合物显示出强有力的抗念珠菌活性，上级优于咪康唑和其他临床感兴趣的抗真菌药物。1-（4-氯苯基）-1-（2，4-二氯苯氧基）-3-（1H-咪唑-1-基）丙烷（16）是试验咪唑类中活性最高的，其活性约为咪康唑的2倍，细胞毒性也远低于咪康唑。甲基、硝基、氟和氯（Cl > F > CH（3）> NO（2）> CF（3））均能使活性显著提高。
Imidazole analogues of fluoxetine have been obtained by replacing the methylamino terminus of aminopropane chain with the imidazole ring. The newly designed imidazoles showed potent anti-Candida activity, superior to those of miconazole and other antifungal agents of clinical interest. 1-(4-Chlorophenyl)-1-(2,4-dichlorophenoxy)-3-(1H-imidazol-1-yl)propane (16), the most active among test imidazoles, was about 2-fold more active and as much less cytotoxic than miconazole. High increase of activity was observed with methyl, nitro, fluorine, and chlorine (Cl > F > CH(3) > NO(2) > CF(3)).