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A Medicinal Chemistry Perspective on 4-Aminoquinoline Antimalarial Drugs

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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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Keywords: Plasmodium falciparum chloroquine resistance transporter (PfCRT); antimalarial; chloroquine (CQ) resistance; combinatorial chemistry; drug-design; drug-metabolism; plasmodium falciparum

Document Type: Research Article

Affiliations: Departments of Chemistry and of Pharmacology, The Robert Robinson Laboratories, University of Liverpool, Liverpool L69 7ZD, United Kingdom.

Publication date: 01 March 2006

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