Posner Gary H, Paik Ik-Hyeon, Chang Wonsuk, Borstnik Kristina, Sinishtaj Sandra, Rosenthal Andrew S, Shapiro Theresa A
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins Malaria Research Institute, Johns Hopkins University, Baltimore, Maryland 21218, USA.
J Med Chem. 2007 May 17;50(10):2516-9. doi: 10.1021/jm070149m. Epub 2007 Apr 17.
We disclose here for the first time the curative activity of a new generation of trioxane dimers, designed logically and prepared easily from the natural trioxane artemisinin in only four or five chemical steps that would be easily accomplished also on a manufacturing scale. Four of these trioxane dimers cure malaria-infected mice after only a single subcutaneous dose, and two other dimers cure after three oral doses.
我们首次在此披露新一代三恶烷二聚体的治疗活性,其设计合理,仅通过四到五步化学反应就能从天然三恶烷青蒿素轻松制备,这些步骤在生产规模上也很容易实现。其中四种三恶烷二聚体仅单次皮下给药后就能治愈感染疟疾的小鼠,另外两种二聚体经三次口服给药后可治愈。