Leishmaniasis is an infectious disease caused by protozoan parasites of the genus Leishmania. The treatment of all forms of leishmaniasis relies on first-line drug, pentavalent antimonial, and in cases of drug failure, the second-line drug amphotericin B has been used. Besides the high toxicity of drugs, parasites can be resistant to antimonial in some areas of the World, making it necessary to perform further studies for the characterization of new antileishmanial agents. Thus, the aim of the present work was to evaluate the leishmanicidal activity of tolnaftate, a selective reversible and non-competitive inhibitor of the fungal enzyme squalene epoxidase, which is involved in the biosynthesis of ergosterol, essential to maintain membrane physiology in fungi as well as trypanosomatids. Tolnaftate eliminated promastigote forms of L. (L.) amazonensis, L. (V.) braziliensis and L. (L.) infantum (EC₅₀ ~ 10 μg/mL and SI ~ 20 for all leishmanial species), and intracellular amastigote forms of all studied species (EC₅₀ ~ 23 μg/mL in infections caused by dermatotropic species; and 11.7 μg/mL in infection caused by viscerotropic species) with high selectivity toward parasites [SI ~ 8 in infections caused by dermatotropic species and 17.4 for viscerotropic specie]. Promastigote forms of L. (L.) amazonensis treated with the EC₅₀ of tolnaftate displayed morphological and physiological changes in the mitochondria and cell membrane. Additionally, promastigote forms treated with tolnaftate EC₅₀ reduced the level of ergosterol by 5.6 times in comparison to the control parasites. Altogether, these results suggest that tolnaftate has leishmanicidal activity towards Leishmania sp., is selective, affects the cell membrane and mitochondria of parasites and, moreover, inhibits ergosterol production in L. (L.) amazonensis.

利什曼病是由属原生动物寄生虫传染病利什曼原虫。所有形式的利什曼病的治疗都依赖于一线药物，五价锑，在药物衰竭的情况下，已经使用了两线药物两性霉素B。除了药物的高毒性外，在世界某些地区，寄生虫还可以对锑产生抗药性，因此有必要进行进一步的研究以鉴定新的抗疟药。因此，本研究的目的是评估甲苯磺酸酯的杀真菌活性，甲苯磺酸酯是一种选择性的可逆且非竞争性的真菌角鲨烯环氧酶抑制剂，它参与麦角固醇的生物合成，这对于维持真菌的膜生理也是必不可少的。作为锥虫。Tolnaftate消除了亚马逊L.（L.）和巴西L.（V.）的前鞭毛体形式L.（L.）婴儿（EC ₅₀  〜10μg/ mL和SI〜20的所有利什曼原虫种），和所有研究的物种的细胞内无鞭毛体形式（EC ₅₀  〜23微克/毫升引起dermatotropic物种感染;和11.7内生菌种引起的感染的微克/毫升）对寄生虫具有高选择性[由亲生菌种引起的感染的SI〜8，对内生菌种的感染为17.4]。用托拉夫特的EC ₅₀处理的亚马逊L.（L.）亚马逊前鞭毛体形式在线粒体和细胞膜中表现出形态和生理变化。此外，用托萘酯EC ₅₀处理过的前鞭毛体形式与对照寄生虫相比，麦角固醇水平降低了5.6倍。总而言之，这些结果表明甲苯磺酸盐具有对利什曼原虫的利什曼杀菌活性，具有选择性，影响寄生虫的细胞膜和线粒体，此外，还抑制了亚马逊L.（L。）的麦角固醇的产生。