Abstract
A broad overview is presented describing the current knowledge and the ongoing research concerning the 4- aminoquinolines (4AQ) as chemotherapeutic antimalarial agents. Included are discussions of mechanism of action, structure activity relationships (SAR), chemistry, metabolism and toxicity and parasite resistance mechanisms. In discussions of SAR, particular emphasis has been given to activity versus chloroquine resistant strains of Plasmodium falciparum. Promising new lead compounds undergoing development are described and an overview of physicochemical properties of chloroquine and amodiaquine analogues is also included.
Keywords: plasmodium falciparum, combinatorial chemistry, drug-metabolism, drug-design, chloroquine (CQ) resistance, antimalarial, Plasmodium falciparum chloroquine resistance transporter (PfCRT)
Current Topics in Medicinal Chemistry
Title: A Medicinal Chemistry Perspective on 4-Aminoquinoline Antimalarial Drugs
Volume: 6 Issue: 5
Author(s): Patrick G. Bray, B. K. Park, Egbaleh Asadollaly, Giancarlo A. Biagini, J. P. Jeyadevan, Neil G. Berry, Stephen A. Ward and Paul M. O' Neill
Affiliation:
Keywords: plasmodium falciparum, combinatorial chemistry, drug-metabolism, drug-design, chloroquine (CQ) resistance, antimalarial, Plasmodium falciparum chloroquine resistance transporter (PfCRT)
Abstract: A broad overview is presented describing the current knowledge and the ongoing research concerning the 4- aminoquinolines (4AQ) as chemotherapeutic antimalarial agents. Included are discussions of mechanism of action, structure activity relationships (SAR), chemistry, metabolism and toxicity and parasite resistance mechanisms. In discussions of SAR, particular emphasis has been given to activity versus chloroquine resistant strains of Plasmodium falciparum. Promising new lead compounds undergoing development are described and an overview of physicochemical properties of chloroquine and amodiaquine analogues is also included.
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Bray G. Patrick, Park K. B., Asadollaly Egbaleh, Biagini A. Giancarlo, Jeyadevan P. J., Berry G. Neil, Ward A. Stephen and O' Neill M. Paul, A Medicinal Chemistry Perspective on 4-Aminoquinoline Antimalarial Drugs, Current Topics in Medicinal Chemistry 2006; 6 (5) . https://dx.doi.org/10.2174/156802606776743147
DOI https://dx.doi.org/10.2174/156802606776743147 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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