ACTIVITY OF IMIDAZOLES AGAINST LEISHMANIA-TROPICA IN HUMAN MACROPHAGE CULTURES
ACTIVITY OF IMIDAZOLES AGAINST LEISHMANIA-TROPICA IN HUMAN MACROPHAGE CULTURES
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DOI：
10.4269/ajtmh.1981.30.566
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发表时间：
1981-01-01
影响因子：
3.3
通讯作者：
BERMAN, JD
中科院分区：
文献类型：
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作者：
BERMAN, JD
测定了4种咪唑类化合物在L.热带感染的人单核细胞衍生的巨噬细胞培养物。其中一种咪唑类化合物，即水解酮康唑[顺式-1-{4-[2-（2，4-二氯苯基）-2-（1H-咪唑-1-基甲基）-1，3-二氧戊环-4-基]甲氧基苯基}哌嗪]，在体内可通过结构相似的化合物酮康唑达到的药物浓度（2.0和2.5 μ g/ml）下，可消除80%和95%的寄生虫。咪唑在模型系统中明显具有抗利什曼原虫活性，应考虑将水解酮康唑用于疾病动物模型的体内试验。
The anti-leishmanial activity of 4 imidazoles was determined in L. tropica-infected human monocyte-derived macrophage cultures. One of the imidazoles, hydrolyzed ketoconazole [cis-1-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxyphenyl}piperazine], eliminated 80 and 95% of the parasites at drug concentrations (2.0 and 2.5 .mu.g/ml) achievable in vivo by a structurally similar compound, ketoconazole. An imidazole evidently has anti-leishmanial activity in a model system and hydrolyzed ketoconazole should be considered for in vivo trials in animal models of the disease.