A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs |
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| Authors: | O'Neill Paul M Ward Stephen A Berry Neil G Jeyadevan J Prince Biagini Giancarlo A Asadollaly Egbaleh Park B Kevin Bray Patrick G |
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| Affiliation: | Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool L67 7ZD UK. P.M.oneill01@liv.ac.uk |
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| 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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