Muth Mathias, Hoerr Verena, Glaser Melanie, Ponte-Sucre Alicia, Moll Heidrun, Stich August, Holzgrabe Ulrike
Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Wuerzburg, Germany.
Bioorg Med Chem Lett. 2007 Mar 15;17(6):1590-3. doi: 10.1016/j.bmcl.2006.12.088. Epub 2007 Jan 4.
Sleeping sickness caused by Trypanosoma brucei gambiense and rhodesiense is fatal if left untreated. Due to the toxicity of drugs currently used and the emerging resistance against these drugs new lead compounds are urgently needed. Within the frame of a broad screening program for drugs with antitrypanosomal activity, some highly potent tertiary and quaternary mono- and bisnaphthalimides being active in the lower micromolar and nanomolar range of concentration have been identified. These compounds are easily available via a two- or three-step microwave-driven synthesis with high yield.
由布氏冈比亚锥虫和罗德西亚锥虫引起的昏睡病如果不治疗会致命。由于目前使用的药物具有毒性以及对这些药物出现的耐药性，迫切需要新的先导化合物。在一项针对具有抗锥虫活性药物的广泛筛选计划框架内，已鉴定出一些在低微摩尔和纳摩尔浓度范围内具有活性的高效叔胺和季铵单萘二甲酰亚胺及双萘二甲酰亚胺。这些化合物可通过两步或三步微波驱动合成轻松获得，产率很高。
