This review provides an update of significant advances in the discovery of
peroxidic antimalarial agents, covering the patent and corresponding scient
ific literature from late 1998 to early 2001. Many efforts have been direct
ed towards producing new chemical entities with enhanced chemical stability
and oral activity. In addition, new strategies are being explored, such as
polychemotherapy and chimeric therapy, which may hold considerable promise
in fighting drug resistance. Providing drug candidates with appropriate ph
ysicochemical, pharmacokinetic and biopharmaceutical properties presents an
enormous challenge for the current antimalarial research enterprise, which
lacks significant industrial input.