Current progress in the chemistry, medicinal chemistry and drug design of artemisinin based antimalarials.

This review covers developments in relation to artemisinin-based antimalarial agents. Topics covered include a brief introduction to the history and treatment of malaria, and more recently, drug resistant malaria; the discovery of the naturally occurring novel peroxidic antimalarial artemisinin; artemisinin biosynthesis, metabolism and biotransformations; the diversity of proposed mechanisms of action; pharmacokinetics; the insight into structure-toxicity relationships; the total syntheses and the progress made in the syntheses of its analogs; and, ultimately the contribution of these efforts towards rational drug design in order to access potent, non-toxic antimalarial drugs based on artemisinin.