Antimalarial acridines: Synthesis, in vitro activity against P. falciparum and interaction with hematin

…, B Pradines, T Cresteil, M Perrée-Fauvet…

Index: Guetzoyan, Lucie; Yu, Xiao-Min; Ramiandrasoa, Florence; Pethe, Stephanie; Rogier, Christophe; Pradines, Bruno; Cresteil, Thierry; Perree-Fauvet, Martine; Mahy, Jean-Pierre Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 23 p. 8032 - 8039

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Citation Number: 36

Abstract

A series of acridine derivatives were synthesised and their in vitro antimalarial activity was evaluated against one chloroquine-susceptible strain (3D7) and three chloroquine-resistant strains (W2, Bre1 and FCR3) of Plasmodium falciparum. Structure–activity relationship showed that two positives charges as well as 6-chloro and 2-methoxy substituents on the acridine ring were required to exert a good antimalarial activity. The best compounds ...