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Current Topics in Medicinal Chemistry

Volume 12 Issue 5
ISSN: 1568-0266
eISSN: 1873-5294

 

   All Titles

  Reversed Chloroquine Molecules as a Strategy to Overcome Resistance in Malaria
  pp.400-407 (8) Author: David H. Peyton
 
 
      Abstract

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.

 
  Keywords: Antimalarial, chloroquine, Plasmodium falciparum, drug development, drug design, structure activity relationship, malaria, drug resistance, Reversed Chloroquine drugs (RCQs), combination therapies
  Affiliation: Department of Chemistry, Portland State University, Portland, OR 97207-0751.
 
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