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

Abstract

Because of expanding resistance to efficient and affordable antimalarial drugs likechloroquine, the search is continuing for more effective drugs against this disease. In-vitroantiplasmodial activity and cytotoxicity of α-(acyloxy)-α-(quinolin-4-yl) acetamides onPlasmodium falciparum and structure-activity relationships of this new class of Passeriniadducts is described. The in-vitro antiplasmodial activity of compounds was tested againstchloroquine sensitive 3D7 strain. Toxicity of active compounds was investigated on HepG2cell line. Compounds 1, 20 and 22 showed significant antiplasmodial activity with IC50 valueof 1.511, 1.373 and 1.325 μM, respectively. The active compounds did not show noticeabletoxicity when tested against HepG2 cell line. The present results bring essential elementswhich will be used for the synthesis of more active derivatives of α-(acyloxy)-α-(quinolin-4-yl)acetamides.