Glutathione Derivatives Active against Trypanosoma brucei rhodesiense and T. brucei brucei In Vitro
- 1 February 2002
- journal article
- Published by American Society for Microbiology in Antimicrobial Agents and Chemotherapy
- Vol. 46 (2) , 434-437
- https://doi.org/10.1128/aac.46.2.434-437.2002
Abstract
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 (ED 50 ) of 0.2 μM. A quantitative structure activity regression equation relating the log (1/ED 50 ) 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.Keywords
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