Evaluation of Novel α-(Acyloxy)-α-(Quinolin-4-yl) Acetamides as Antiplasmodial Agents.

Because of expanding resistance to efficient and affordable antimalarial drugs like chloroquine, the search is continuing for more effective drugs against this disease. In-vitro antiplasmodial activity and cytotoxicity of α-(acyloxy)-α-(quinolin-4-yl) acetamides on Plasmodium falciparum and structure-activity relationships of this new class of Passerini adducts is described. The in-vitro antiplasmodial activity of compounds was tested against chloroquine sensitive 3D7 strain. Toxicity of active compounds was investigated on HepG2 cell line. Compounds 1, 20 and 22 showed significant antiplasmodial activity with IC50 value of 1.511, 1.373 and 1.325 µM, respectively. The active compounds did not show noticeable toxicity when tested against HepG2 cell line. The present results bring essential elements which will be used for the synthesis of more active derivatives of α-(acyloxy)-α-(quinolin-4-yl) acetamides.