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Antimicrobial Agents and Chemotherapy, December 2005, p. 5169-5171, Vol. 49, No. 12
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.12.5169-5171.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.

Interaction of Monobenzamidine-Linked Trypanocides with the Trypanosoma brucei P2 Aminopurine Transporter

Mhairi L. Stewart,1 Cyrille Boussard,2 Reto Brun,3 Ian H. Gilbert,2 and Michael P. Barrett1*

University of Glasgow, Institute of Biomedical and Life Sciences, Division of Infection and Immunity, Glasgow G12 8QQ, United Kingdom,1 Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3XF, United Kingdom,2 Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland3

Received 23 August 2005/ Returned for modification 16 September 2005/ Accepted 3 October 2005

Single benzamidine group-carrying compounds were shown to interact with the Trypanosoma brucei P2 aminopurine transporter. Replacement of the amidine with a guanidine group decreased affinity. Trypanocidal activity was evident, but compounds were equally toxic against trypanosomes lacking the P2 transporter, which indicates additional uptake routes for monobenzamidine-derived compounds.

* Corresponding author. Mailing address: University of Glasgow, Institute of Biomedical and Life Sciences, Division of Infection & Immunity, Glasgow G12 8QQ, United Kingdom. Phone and fax: 44-141-330-6904. E-mail: m.barrett{at}bio.gla.ac.uk.

Antimicrobial Agents and Chemotherapy, December 2005, p. 5169-5171, Vol. 49, No. 12
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.12.5169-5171.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Sykes, M. L., Avery, V. M. (2009). Development of an Alamar BlueTM Viability Assay in 384-Well Format for High Throughput Whole Cell Screening of Trypanosoma brucei brucei Bloodstream Form Strain 427. Am J Trop Med Hyg 81: 665-674 [Abstract] [Full Text]  


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