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Antimicrobial Agents and Chemotherapy, February 2002, p. 434-437, Vol. 46, No. 2
0066-4804/01/$04.00+0     DOI: 10.1128/AAC.46.2.434-437.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

Glutathione Derivatives Active against Trypanosoma brucei rhodesiense and T. brucei brucei In Vitro

Department of Chemistry & Materials, The Manchester Metropolitan University, Manchester M1 5GD, United Kingdom

Received 30 July 2001/ Returned for modification 20 September 2001/ Accepted 10 November 2001

Diesters based on N-benzyloxycarbonyl-S-(2,4-dinitrophenyl) GSH (CBzGSDNP) containing linear alcohols 3 to 9, branched alcohols 10 to 20, or heteroatom linear alcohols 21 to 25, were investigated as in vitro inhibitors of pathogenic parasites. Diesters 3 to 25 were better inhibitors of Trypanosoma brucei rhodesiense than of T. brucei brucei and had low cytotoxicities. The most active compound had a 50% effective dose (ED₅₀) of 0.2 µM. A quantitative structure activity regression equation relating the log (1/ED₅₀) versus the hydrophobicity parameter (log P), Taft's steric parameter (E_s), molecular weight (MW), and the WienI descriptor (W) was determined, and the species difference was found to be related to membrane penetration and steric effects.