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JAC Advance Access originally published online on July 1, 2003
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Journal of Antimicrobial Chemotherapy (2003) 52, 290-293
© 2003 The British Society for Antimicrobial Chemotherapy

Antiplasmodial activity of a series of 1,3,5-triazine-substituted polyamines

Burkhard Klenke1, Michael P. Barrett2, Reto Brun3 and Ian H. Gilbert1,*

1 Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3XF; 2 Institute of Biomedical and Life Sciences, Division of Infection and Immunity, University of Glasgow, Glasgow G12 8QQ, UK; 3 Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland

Received 30 August 2002; returned 10 January 2003; revised 23 January 2003; accepted 29 April 2003

Polyamine biosynthesis and function has been shown to be a good drug target in some parasitic protozoa and it is proposed that the pathway might also represent a target in the malaria parasite Plasmodium falciparum. A series of 1,3,5-triazine-substituted polyamine analogues were tested for activity against Plasmodium falciparum in vitro. The series showed activity against the parasites and were generally more active against the chloroquine-resistant line K1 than the chloroquine-susceptible line NF54. Simple unbranched analogues had better activity than analogues carrying branched or cyclic central chains. Addition of multiple triazine units in general led to increased activity of the compounds.

Keywords: Plasmodium falciparum, malaria, parasites, protozoa, polyamine metabolism

* Corresponding author. Tel: +44-29-2087-5800; Fax: +44-29-2087-4149; E-mail: gilbertih{at}cf.ac.uk


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