2-氨基环己醇和1,2-环己二胺衍生物的抗利什曼原虫和抗锥虫活性
Leishmanicidal and trypanocidal activities of 2-aminocyclohexanol and 1,2-cyclohexanediamine derivatives.
作者信息
Rebollo Oscar, del Olmo Esther, Ruiz Grace, López-Pérez José L, Giménez Alberto, San Feliciano Arturo
机构信息
Departamento de Química Farmacéutica, Facultad de Farmacia, CIETUS, Universidad de Salamanca, Salamanca, Spain.
出版信息
Bioorg Med Chem Lett. 2008 Jan 1;18(1):184-7. doi: 10.1016/j.bmcl.2007.10.102. Epub 2007 Nov 1.
A number of aminoalcohols, diamines and other related cycloanalogues of sphingosine have been synthesized and assayed in vitro against three Leishmania spp. and Trypanosoma cruzi. Most of the compounds were potent parasiticides, with IC50 values in the microM or lower range and potencies higher than those of pentamidine and benznidazol, the common therapeutic agents against these parasitoses.
已经合成了多种鞘氨醇的氨基醇、二胺及其他相关环类似物，并在体外针对三种利什曼原虫和克氏锥虫进行了测定。大多数化合物都是有效的杀寄生虫剂，其半数抑制浓度（IC50）值在微摩尔或更低范围内，效力高于喷他脒和苄硝唑，这两种是治疗这些寄生虫病的常用药物。
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