title: A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs.
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.
authors.affiliation: Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool L67 7ZD UK. P.M.oneill01@liv.ac.uk
authors.forename: Paul M
authors.initials: PM
authors.lastname: O'Neill
authors.forename: Stephen A
authors.initials: SA
authors.lastname: Ward
authors.forename: Neil G
authors.initials: NG
authors.lastname: Berry
authors.forename: J Prince
authors.initials: JP
authors.lastname: Jeyadevan
authors.forename: Giancarlo A
authors.initials: GA
authors.lastname: Biagini
authors.forename: Egbaleh
authors.initials: E
authors.lastname: Asadollaly
authors.forename: B Kevin
authors.initials: BK
authors.lastname: Park
authors.forename: Patrick G
authors.initials: PG
authors.lastname: Bray
mesh_terms: D000634:Aminoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000655:Amodiaquine / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002738:Chloroquine / Q000737:chemistry / Q000494:pharmacology; D004351:Drug Resistance; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D000655:Amodiaquine; D002738:Chloroquine; C001920:4-aminoquinoline