Laboratoire de Chimie de Coordination du CNRS, Toulouse, France.
J Med Chem. 2010 May 27;53(10):4103-9. doi: 10.1021/jm100117e.
The synthesis, characterization, and antimalarial evaluation of a new series of potential antimalarial molecules, named trioxaferroquines, are reported. Trioxaferroquines are hybrid antimalarial drugs containing a 1,2,4-trioxane covalently linked to ferroquine (Fq), a synthetic ferrocenylquinoline derivative currently under clinical development. The aim was to combine, within a single structure, an iron(II) species, a 1,2,4-trioxane, as in artemisinin, and a substituted quinoline, as in chloroquine.
报道了一系列新型潜在抗疟分子——三氧杂铁喹啉的合成、表征和抗疟评价。三氧杂铁喹啉是一种杂合抗疟药物,含有一个 1,2,4-三氧杂环己烷与铁喹啉(Fq)共价连接,Fq 是一种目前正在临床开发的合成铁菲咯啉衍生物。目的是在一个单一结构中结合铁(II)物种、1,2,4-三氧杂环己烷(如青蒿素)和取代的喹啉(如氯喹)。