Medicinal Organometallic Chemistry

Volume 32 of the series Topics in Organometallic Chemistry pp 155-193


Bioorganometallic Chemistry and Malaria

  • Christophe BiotAffiliated withUnité de Catalyse et de Chimie du Solide – UMR CNRS 8181, ENSCL, Université de Lille 1Unité de Glycobiologie Structurale et Fonctionnelle – UMR CNRS 8576, Université de Lille 1 Email author 
  • , Daniel DiveAffiliated withInserm U547, Institut Pasteur, Université Lille Nord de France

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This chapter summarizes recent developments in the design, synthesis, and structure–activity relationship studies of organometallic antimalarials. It begins with a general introduction to malaria and the biology of the parasite Plasmodium falciparum, with a focus on the heme detoxification system. Then, a number of metal complexes from the literature are reported for their antiplasmodial activity. The second half of the chapter deals with the serendipitous discovery of ferroquine, its mechanism(s) of action, and the failure to induce a resistance. Last, but not least, we suggest that the bioorganometallic approach offers the potential for the design of novel therapeutic agents.


Antimalarial Bioorganometallic Drug resistance ferroquine