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Full-Text Articles in Medicinal-Pharmaceutical Chemistry
New 4-Aminoquinoline Compounds To Reverse Drug Resistance In P. Falciparum Malaria, And A Survey Of Early European Antimalarial Treatments, Katherine May Liebman
New 4-Aminoquinoline Compounds To Reverse Drug Resistance In P. Falciparum Malaria, And A Survey Of Early European Antimalarial Treatments, Katherine May Liebman
Dissertations and Theses
Intermittent fevers caused by Plasmodium parasites have been known for millennia, and have caused untold human suffering. Today, millions of people are afflicted by malaria each year, and hundreds of thousands die. Historically, the most successful synthetic antimalarial drug was chloroquine, as it was safe, inexpensive, and highly efficacious. However, plasmodial resistance to chloroquine now greatly limits its utility. Previously in our laboratories it has been shown that attachment of a "reversal agent moiety" to the side chain of chloroquine can result in the restoration of activity against chloroquine-resistant strains of P. falciparum malaria. In the first part of the …
Reversed Chloroquine Molecules As A Strategy To Overcome Resistance In Malaria, David H. Peyton
Reversed Chloroquine Molecules As A Strategy To Overcome Resistance In Malaria, David H. Peyton
Chemistry Faculty Publications and Presentations
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.