Targeted delivery of compounds to Trypanosoma brucei using the melamine motif

Chollet, C., Baliani, A., Wong, P.E., Barrett, M.P. and Gilbert, I.H. (2009) Targeted delivery of compounds to Trypanosoma brucei using the melamine motif. Bioorganic and Medicinal Chemistry, 17(6), pp. 2512-2523. (doi:10.1016/j.bmc.2009.01.058)

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Publisher's URL: http://dx.doi.org/10.1016/j.bmc.2009.01.058

Abstract

There is an urgent need for the development of new drugs for the treatment of human African trypanosomiasis. The causative organism, Trypanosoma brucei, has been shown to have some unusual plasma membrane transporters, in particular the P2 aminopurine transporter and related permeases, which have been used for the selective targeting of trypanocidal compounds to the organism. In this paper, we report the addition of melamine-based P2-targeting motifs to three different classes of compound in order to try and improve activity through increased selective uptake. The classes reported here are fluoroquinolones, difluoromethylornithine and artesunate derivatives.

Item Type:Articles
Keywords:Trypanosoma brucei, delivery, melamine, eflornithine, fluoroquinolones
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Barrett, Professor Michael
Authors: Chollet, C., Baliani, A., Wong, P.E., Barrett, M.P., and Gilbert, I.H.
Subjects:Q Science > QD Chemistry
Q Science > QH Natural history > QH345 Biochemistry
Q Science > QP Physiology
College/School:College of Medical Veterinary and Life Sciences
College of Medical Veterinary and Life Sciences > Institute of Infection Immunity and Inflammation
Journal Name:Bioorganic and Medicinal Chemistry
ISSN:0968-0896

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