Two new series of 28 selenocyanate and diselenide derivatives containing amide moieties were designed, synthesized, and evaluated for their leishmanicidal activity against
Leishmania infantum
axenic amastigotes, and selectivity was assessed in human THP-1 cells. Eleven compounds exhibited excellent leishmanicidal activity with EC
50
values lower than the reference drug miltefosine (EC
50
= 2.84 μM). In addition, for six of them the selectivity index ranged from 9 to >1,442, greater than both references used.
设计、合成并评估了两个新系列的 28 种含酰胺分子的硒氰酸酯和二硒化物衍生物对婴儿利什曼原虫的杀利什曼活性。
婴儿利什曼病
的杀利什曼活性,并在人 THP-1 细胞中进行了选择性评估。11 个化合物表现出优异的杀利什曼活性,EC
50
值低于参考药物米替福新(EC
50
= 2.84 μM)。此外,其中六个化合物的选择性指数在 9 到 1442 之间,高于所用的两种参考药物。