Phenotypic assay against Leishmania amazonensis in vitro and in vivo led to identification of an adamantyl-based phenyl sulfonyl acetamide (compound 1) as a promising antileishmanial agent. Compound 1 inhibited the growth of intracellular forms of L. amazonensis (50% inhibitory concentration [IC₅₀] = 4 μM) and exhibited low toxicity to host cells, with a selectivity index (SI) of >125. However, in a cutaneous leishmaniasis (CL) mouse model, compound 1 did not reduce lesions and parasite load when administered as monotherapy or when given simultaneously with a suboptimal dose of miltefosine.

中文翻译：

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基于金刚烷基的苯基磺酰基乙酰胺对亚马逊乳杆菌皮肤利什曼病模型的体外和体内评价。

在体外和体内对亚马逊利什曼原虫的 表型测定导致基于金刚烷基的苯基磺酰基乙酰胺（化合物1）的鉴定为一种有希望的抗菌剂。化合物1抑制了亚马孙乳杆菌的细胞内形式的生长（50％抑制浓度[IC ₅₀ ] = 4μM），并且对宿主细胞的毒性低，选择性指数（SI）> 125。但是，在皮肤利什曼病（CL）小鼠模型中，化合物1作为单药治疗或与次优剂量的米替福辛同时给药时，并未减轻病灶和寄生虫负荷。