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
Current Topics in Medicinal Chemistry
Title: Reversed Chloroquine Molecules as a Strategy to Overcome Resistance in Malaria
Volume: 12 Issue: 5
Author(s): David H. Peyton
Affiliation:
Keywords: Antimalarial, chloroquine, Plasmodium falciparum, drug development, drug design, structure activity relationship, malaria, drug resistance, Reversed Chloroquine drugs (RCQs), combination therapies
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.
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Cite this article as:
H. Peyton David, Reversed Chloroquine Molecules as a Strategy to Overcome Resistance in Malaria, Current Topics in Medicinal Chemistry 2012; 12 (5) . https://dx.doi.org/10.2174/156802612799362968
DOI https://dx.doi.org/10.2174/156802612799362968 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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