The author thanks The Medical Research Foundation of Oregon (Grant 0530) and the National Institutes of Health (Grants AI067837, AI072923, and AI090848) for financial support.
Current Topics in Medicinal Chemistry
Drug design, Chloroquine -- Antimalarials, Plasmodium falciparum, Malaria
This short review tells the story of how Reversed Chloroquine drugs (RCQs) were developed. These are hybrid molecules, made by combining the quinoline nucleus from chloroquine (CQ) with moieties which are designed to inhibit efflux via known transporters in the membrane of the digestive vacuole of the malaria parasite. The resulting RCQ drugs can have potencies exceeding that of CQ, while at the same time having physical chemical characteristics that may make them favorable as partner drugs in combination therapies. The need for such novel antimalarial drugs will continue for the foreseeable future.
Peyton, David H. "Reversed Chloroquine Molecules as a Strategy to Overcome Resistance in Malaria." Current Topics in Medicinal Chemistry 12, no. 5 (2012): 400.