Glutathione Derivatives Active against Trypanosoma brucei rhodesiense and T. brucei brucei In Vitro
AUTOR(ES)
Daunes, Sylvie
FONTE
American Society for Microbiology
RESUMO
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 (Es), 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.
ACESSO AO ARTIGO
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=127061Documentos Relacionados
- Cultivation in a semi-defined medium of animal infective forms of Trypanosoma brucei, T. equiperdum, T. evansi, T. rhodesiense and T. gambiense.
- Feeder layer-free in vitro assay for screening antitrypanosomal compounds against Trypanosoma brucei brucei and T. b. evansi.
- In Vitro and In Vivo Activities of Aminoadamantane and Aminoalkylcyclohexane Derivatives against Trypanosoma brucei
- Cell-Mediated Hypersensitivity in Rabbits Infected with Trypanosoma brucei and Trypanosoma rhodesiense
- Activity of 2-acetylpyridine thiosemicarbazones against Trypanosoma rhodesiense in vitro.