Influence of Substituents on the Antiplasmodial and Cytotoxic Activities of 5-chloro-3,4-dihydro-1H-pyrano[3,4-b]-1,10-phenanthrolinone as Antimalarial Agent

Abstract

Background: Malaria is one of the most common parasitic disease in tropical and subtropical regions. Plasmodium falciparum, one of the causative agent of malaria is resistant to many type of antimalarial drugs. This study present in vitro assessment of the antiplasmodial activity of substituted phénanthrolinone compounds. Methods: A series of 7 substituents were used to substitute the chlorine on the 5 position in the 5-chloro-3,4-dihydro-1H-pyrano[3,4-b]-1,10-phenanthrolinone ring. In vitro antiplasmodial activities were evaluated on chloroquine-sensitive and resistant strains of P. falciparum. Results: The results showed that compounds 7 and 8 possessing N,N-diethylamino side chain had the best antiplasmodial activities. In addition, the cytotoxic activities were evaluated on HeLa cells and compound 8 was the least cytotoxic of all studied compounds. Conclusion: The synthesis and antimalarial activity of substituents of compound 2 were carried out. This study has shown that compounds with basic and lipophilic substituents exhibited the best antiplasmodial activity.