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A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs

O'Neill, P. M., Ward, Stephen ORCID: https://orcid.org/0000-0003-2331-3192, Berry, N. G., Jeyadevan, J. P., Biagini, Giancarlo ORCID: https://orcid.org/0000-0001-6356-6595, Asadollaly, E., Park, B. K. and Bray, Patrick (2006) 'A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs'. Current Topics in Medicinal Chemistry, Vol 6, Issue 5, pp. 479-507.

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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.

Item Type: Article
Uncontrolled Keywords: antimalarial chloroquine (cq) resistance drug-design drug-metabolism combinatorial chemistry plasmodium falciparum plasmodium falciparum chloroquine resistance transporter (pfcrt) activity in-vitro resistant plasmodium-falciparum digestive vacuolar ph drug/metabolite transporter superfamily transmembrane protein pfcrt mannich base antimalarials metal-based chemotherapy chloroquine resistance malaria parasites physicochemical properties
Subjects: QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials
QV Pharmacology > QV 38 Drug action.
QX Parasitology > Protozoa > QX 135 Plasmodia
Faculty: Department: Groups (2002 - 2012) > Molecular & Biochemical Parasitology Group
Depositing User: Martin Chapman
Date Deposited: 07 Mar 2011 15:11
Last Modified: 06 Feb 2018 13:02
URI: http://archive.lstmed.ac.uk/id/eprint/1569

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