Leishmaniasis is an infectious disease with several limitations regarding treatment schemes. This work reports the anti-Leishmania activity of spiroacridine compounds against the promastigote (IC₅₀ = 1.1 to 6.0 µg / mL) and amastigote forms of the best compounds (EC₅₀ = 4.9 and 0.9 µg / mL) in Leishmania (L.) infantum and proposes an in-silico study with possible selective therapeutic targets for L. infantum. The substituted dimethyl-amine compound (AMTAC 11) showed the best leishmanicidal activity in vitro, and was found to interact with TryR and LdTopoI. comparisons with standard inhibitors were performed, and its main interactions were elucidated. Based on the biological assessment and the structure-activity relationship study, the spiroacridine compounds appear to be promising anti-leishmania chemotherapeutic agents to be explored.

利什曼病是一种传染病，在治疗方案方面存在一些局限性。这项工作报告了螺吖啶化合物对婴儿利什曼原虫 (L.)中的前鞭毛体 (IC ₅₀  = 1.1 至 6.0 µg/mL) 和最佳化合物的无鞭毛体形式 (EC ₅₀  = 4.9 和 0.9 µg/mL)的抗利什曼原虫活性并提出了一项针对婴儿乳杆菌可能的选择性治疗靶点的计算机内研究。取代的二甲胺化合物 (AMTAC 11)在体外表现出最佳的利什曼原虫活性，并发现与 TryR和    LdTopoI。进行了与标准抑制剂的比较，并阐明了其主要相互作用。根据生物学评估和构效关系研究，螺吖啶化合物似乎是有前景的 抗利什曼原虫 化疗药物。