A Medicinal Chemistry Perspective on 4-Aminoquinoline Antimalarial Drugs

Authors: O' Neill, Paul M.1; Ward, Stephen A.1; Berry, Neil G.1; Jeyadevan, J. P.1; Biagini, Giancarlo A.1; Asadollaly, Egbaleh1; Park, B. K.1; Bray, Patrick G.1

Source: Current Topics in Medicinal Chemistry, Volume 6, Number 5, March 2006 , pp. 479-507(29)

Publisher: Bentham Science Publishers

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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.

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

Document Type: Research article

DOI: 10.2174/156802606776743147

Affiliations: 1: Departments of Chemistry and of Pharmacology, The Robert Robinson Laboratories, University of Liverpool, Liverpool L69 7ZD, United Kingdom.

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