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

Document Type: Research article

Authors

1 Zanjan Pharmaceutical Biotechnology Research Center, Zanjan University of Medical Sciences, Zanjan, Iran

2 Department of Chemistry, University of Zanjan, Zanjan, Iran.

Abstract

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.

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