A series of thirty-one selenocompounds covering a wide chemical space was assessed for in vitro leishmanicidal activities against Leishmania infantum amastigotes. The cytotoxicity of those compounds was also evaluated on human THP-1 cells. Interestingly most tested derivatives were active in the low micromolar range and seven of them (A.I.3, A.I.7, B.I.1, B.I.2, C.I.7 C.I.8 and C.II.8) stood out for selectivity indexes higher than the ones exhibited by reference compounds mitelfosine and edelfosine. These leader compounds were evaluated against infected macrophages and their trypanothione reductase (TryR) inhibition potency was measured to further approach the mechanism by which they caused their action. Among them diselenide tested structures were pointed out for their ability to reduce infection rates. Three of the leader compounds inhibited TryR effectively, therefore this enzyme may be implicated in the mechanism of action by which these compounds cause their leishmanicidal effect.

一系列的31硒化合物覆盖面广化学品空间被评定为体外leishmanicidal对活动婴儿利什曼原虫无鞭毛体。还评估了这些化合物对人THP-1细胞的细胞毒性。有趣的是，大多数经过测试的衍生物在低微摩尔范围内均具有活性，其中有七个（AI3，AI7，BI1，BI2，CI7，CI8和C.II.8）。）的选择性指数高于参考化合物米替福星和依德福星所显示的那些。对这些先导化合物进行了抗感染巨噬细胞的评估，并测定了其锥虫硫醚还原酶（TryR）的抑制能力，以进一步接近其引起其作用的机理。其中指出了经二硒化物测试的结构降低感染率的能力。前导化合物中的三种有效地抑制了TryR，因此该酶可能与这些化合物引起其杀菌作用的作用机理有关。