With the aim to identify a potential drug candidate to treat cutaneous leishmaniasis, a series of 1-phthalazinyl hydrazones were synthesized and tested against Leishmania braziliensis parasite, one of the main responsible of this disease in the world. A structure-activity relationship permitted to identify two phthalazines containing nitroheterocyclic moiety 3l and 3m as promising new lead compounds. These compounds showed a significant antileishmanial activity against promastigote form of L. braziliensis, with EC₅₀ values in sub-micromolar and nanomolar ranges. The phthalazine 3l also displayed a selective and excellent activity against the clinically relevant intracellular amastigotes form, with a EC₅₀ value in sub-micromolar range (0.59 μM), without affecting the viability of the host cells. Oxidative stress was identified as the possible mode of action of the most active phthalazine. Considering their significant antileishmanial activity and ease synthesis, the phthalazine containing nitroheterocyclic represents a promising agent against Leishmania braziliensis for the rational design of new leads.

为了确定治疗皮肤利什曼病的潜在候选药物，合成了一系列1-酞嗪基并针对巴西利什曼原虫的寄生虫进行了测试，该寄生虫是世界上导致该病的主要病因之一。构效关系可以确定两种含氮杂环部分3l和3m的酞嗪为有前途的新型先导化合物。这些化合物显示出对前鞭毛体的形式的显著antileishmanial活性L. braziliensis，用EC _50倍在亚微摩尔和纳摩尔范围内的值。酞嗪3l还显示针对临床相关的胞内无鞭毛体形式的选择性和优良的活性，具有EC ₅₀在亚微摩尔范围的值（0.59  μ M），在不影响宿主细胞的生存能力。氧化应激被确定为最具活性的酞嗪的可能作用方式。考虑到它们具有显着的抗菌活性和易于合成的特性，因此，对于硝基苯的合理设计，含有硝基杂环的酞嗪代表了一种有希望的抗巴西利什曼原虫的试剂。