Metallocene-based antimalarials: An exploration into the influence of the ferrocenyl moiety on in vitro antimalarial activity in chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum


Blackie, MAL; Beagley, P; Croft, SL; Kendrick, H; Moss, JR; Chibale, K; (2007) Metallocene-based antimalarials: An exploration into the influence of the ferrocenyl moiety on in vitro antimalarial activity in chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Bioorganic & medicinal chemistry, 15 (20). pp. 6510-6516. ISSN 0968-0896 DOI: 10.1016/j.bmc.2007.07.012

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Abstract

To establish the role of the ferrocenyl moiety in the antiplasmodial activity of ferroquine, compounds in which this moiety is replaced by the corresponding ruthenium-based moieties were synthesized and evaluated. In both the sensitive (D 10) and resistant (K1) strains of Plasmodium falciparum, ruthenoquine analogues showed comparable potency to ferroquine. This suggests that a probable role of the ferrocenyl fragment is to serve simply as a hydrophobic spacer group. In addition, ferroquine analogues with different aromatic substituents were synthesized and evaluated. Unexpectedly high activity for quinoline compounds lacking the 7-chloro substituent suggests the ferrocenyl moiety may have an additive and/or synergistic effect. (c) 2007 Elsevier Ltd. All rights reserved.

Item Type: Article
Keywords: Animals, Antimalarials, chemical synthesis, chemistry, pharmacology, Chloroquine, chemistry, pharmacology, Drug Resistance, drug effects, Ferrous Compounds, chemistry, Molecular Structure, Organometallic Compounds, chemical synthesis, chemistry, pharmacology, Plasmodium falciparum, drug effects, Sensitivity and Specificity, Structure-Activity Relationship
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Research Centre: Antimicrobial Resistance Centre (AMR)
Malaria Centre
PubMed ID: 17693090
Web of Science ID: 249713900002
URI: http://researchonline.lshtm.ac.uk/id/eprint/8413

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