Delarue-Cochin Sandrine, Grellier Philippe, Maes Louis, Mouray Elisabeth, Sergheraert Christian, Melnyk Patricia
UMR CNRS 8525, Université de Lille II, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447, 59021 Lille cedex, France.
Eur J Med Chem. 2008 Oct;43(10):2045-55. doi: 10.1016/j.ejmech.2007.11.003. Epub 2007 Nov 19.
A series of 4-anilinoquinolines bearing an amino side chain linked to the aromatic ring with a carbamate or an amide bond were synthesized and evaluated for their antimalarial activity and their cytotoxicity upon MRC-5 cells. Among the 17 compounds, a majority was found to be active in the low nanomolar range against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro with relative low cytotoxicity. Two compounds were then tested on mice infected by Plasmodium berghei and were found to exhibit reasonable in vivo activity.
合成了一系列带有通过氨基甲酸酯或酰胺键与芳环相连的氨基侧链的4-苯胺基喹啉，并对其抗疟活性和对MRC-5细胞的细胞毒性进行了评估。在这17种化合物中，大多数在体外对氯喹敏感和耐药的恶性疟原虫菌株具有低纳摩尔范围内的活性，且细胞毒性相对较低。然后对两种化合物在感染伯氏疟原虫的小鼠身上进行了测试，发现它们在体内表现出合理的活性。
