Synthesis, characterization and antimalarial activity of new iridium–chloroquine complexes

Chloroquine base (CQ) reacts with [Ir(COD)Cl]2 and IrCl3 · 3H2O to yield of Ir(CQ)Cl(COD) (1) and Ir2Cl6(CQ) · 3H2O (2), respectively. Reaction of [Ir(COD)Cl]2 with CQ in the presence of NH4PF6 leaded to [Ir(CQ)(Solv)2]PF6 (3). The three new iridium–CQ complexes were characterized by a combination of elemental analysis, IR and NMR spectroscopies and evaluated in vitro against Plasmodium beghei. Comparison of the IC50 values obtained with the experimental compounds with that determined for chloroquine diphosphate indicated a higher activity for complex 2, while complexes 1 and 3 showed a similar and lower activity, respectively.

Three new iridium–chloroquine complexes Ir(CQ)Cl(COD) (1), Ir2Cl6(CQ) · 3H2O (2) and [Ir(CQ)(Solv)2]PF6 (3) were synthesized and testing in vitro against Plasmodium berghei. Comparison of the IC50 values obtained for complexes (1–3) versus parental drug indicated a higher activity for complex 1, while complexes 2 and 3 showed a similar and lower activity, respectively.Figure optionsDownload as PowerPoint slide