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
Cheikh Sall *
Laboratoire de Chimie, UFR des Sciences de la Santé, Université de Thiès, BP 967 Thiès, Sénégal.
Samba Fama Ndoye
Laboratoire de Chimie Organique et Thérapeutique, Faculté de Médecine de Pharmacie et d’Odontologie, Université Cheikh Anta Diop de Dakar, BP 5005 Dakar-Fann, Sénégal.
Matar Seck
Laboratoire de Chimie Organique et Thérapeutique, Faculté de Médecine de Pharmacie et d’Odontologie, Université Cheikh Anta Diop de Dakar, BP 5005 Dakar-Fann, Sénégal.
Alexis Valentin
Université de Toulouse, Pharma-DEV, IRD, Université Paul Sabatier, 31062 Toulouse Cedex 4, France.
Yves Blache
Université de Toulon, MAPIEM, EA 4323, 83957 La Garde, France.
*Author to whom correspondence should be addressed.
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.
Keywords: Malaria disease, Plasmodium falciparum, 1,10-phenanthrolinone, antimalarial activity.