542-10-9 Purity
≥ 98%
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Specification
Yamamoto ES, et al. Bioorganic Chemistry, 2020, 102, 104056.
Tolnaftate was experimentally evaluated as an antileishmanial agent targeting sterol metabolism in Leishmania spp. Promastigote forms of L. amazonensis, L. braziliensis, and L. infantum were cultured in vitro and treated with graded concentrations of tolnaftate to determine leishmanicidal activity, with EC₅₀ values quantified via cell viability assays. Intracellular amastigote assays were conducted using infected macrophages to assess efficacy under physiologically relevant conditions and calculate selectivity indices. To elucidate the mechanism of action, parasites treated at EC₅₀ concentrations underwent ultrastructural analysis, revealing mitochondrial and membrane alterations. Ergosterol content was quantified following drug exposure, demonstrating a marked reduction consistent with squalene epoxidase inhibition. These experimental results confirm tolnaftate's functional application as a sterol biosynthesis inhibitor, directly linking enzymatic blockade to membrane disruption and parasite death in Leishmania models.
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