Synthesis and evaluation of hybrid bis-cationic salts as antimalarial drugs

Stéphanie Ortial (1) , Severine Denoyelle (1) , Sharon Wein (2) , Olivier Berger (1) , Thierry Durand (1) , Roger Escale (1) , Alain Pellet (2) , Henri Vial (2) , Yen Vo-Hoang (1)

1 IBMM - Institut des Biomolécules Max Mousseron [Pôle Chimie Balard]
2 DIMNP - Dynamique des interactions membranaires normales et pathologiques

A new series of hybrid bis-cations has been synthesized as potent antimalarial agents. These drugs share two different cationic heads derived from bis-thiazolium and bis-amidine salts. Structure-activity relationships has been defined and pointed out that the linker plays a prior role for antimalarial activity leading to compounds with significant oral activity.

Mots clés: biological activity; hybrid bis-cations; malaria; phospholipid metabolism; structure activity relationships

Domaines: Chimie organique

Stéphanie Ortial, Severine Denoyelle, Sharon Wein, Olivier Berger, Thierry Durand, et al.. Synthesis and evaluation of hybrid bis-cationic salts as antimalarial drugs. ChemMedChem, 2010, 5 (1), pp.52-55. ⟨10.1002/cmdc.200900427⟩. ⟨hal-00448020⟩