sitamaquine tosylate

Sitamaquine is an antileishmanial agent.1It is active againstL. donovani,L. infantum,L. mexicana,L. braziliensis, andL. tropica(EC50s = 9.5-19.8 μM). It inhibits mitochondrial complex II, also known as succinate dehydrogenase (SDH), in a cell-free assay when used at concentrations ranging from 10 to 200 μM.2Sitamaquine (100 μM) increases intracellular levels of reactive oxygen species (ROS) and decreases intracellular ATP levels, as well as induces phosphatidylserine externalization, chromatin fragmentation, and depolarization of the mitochondrial membrane potential, markers of apoptosis, inL. donovanipromastigotes. 1.López-Martín, C., Pérez-Victoria, J.M., Carvalho, L., et al.Sitamaquine sensitivity in Leishmania species is not mediated by drug accumulation in acidocalcisomesAntimicrob. Agents Chemother.52(11)4030-4036(2008) 2.Carvalho, L.J.M., Luque-Ortega, J.R., López-Martín, C., et al.The 8-aminoquinoline analogue sitamaquine causes oxidative stress in Leishmania donovani promastigotes by targeting succinate dehydrogenaseAntimicrob. Agents Chemother.55(9)4204-4210(2011)

Sitamaquine（又名WR-6026）是一种具有抗利什曼病属性的口服活性8-氨基喹啉类似物。

Sitamaquine hydrochloride (WR 6026)，一种具口服活性的8-aminoquinoline衍生物，能有效抗利什曼病。该化合物主要通过抑制线粒体复合物II（琥珀酸脱氢酶）发挥作用。作为一种嗜脂性弱碱，Sitamaquine hydrochloride 在利什曼原虫的酸性环境中能快速积累，尤其是在酸钙小体内部。