Design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8- chloropyrimido-[4,5-b]quinolines as novel antimalarials

Article abstract of DOI:10.1016/j.bmcl.2004.10.037

The design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8- chloropyrimido-[4,5-b]quinolines as potent antimalarials is reported. Novel 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines were designed based on a pharmacophore developed for potent antimalarial activity using Chem-X and MOE softwares. The designed molecules were synthesized by following a novel route and were evaluated by Rane's test for blood schizonticidal activity in mice infected by Plasmodium berghei. Based on the Mean Survival Time (MST) data, of the nine compounds evaluated, three had curative potential when compared with chloroquine.