期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 12, 页码 3576-3579出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.04.030
关键词
Trypanosoma cruzi; Chagas disease; Disulfide; Carbohydrate
资金
- OTKA K in Hungary [105459]
- CODEI from Antofagasta University [5381]
- [TAMOP-4.2.2.A-11/1/KONV-2012-0025]
Aromatic oligovalent glycosyl disulfides and some diglycosyl disulfides were tested against three different Trypanosoma cruzi strains. Di-(beta-D-galactopyranosyl-dithiomethylene) benzenes 2b and 4b proved to be the most active derivatives against all three strains of cell culture-derived trypomastigotes with IC50 values ranging from 4 to 11 mu M at 37 degrees C. The inhibitory activities were maintained, although somewhat lowered, at a temperature of 4 degrees C as well. Three further derivatives displayed similar activities against at least one of the three strains. Low cytotoxicities of the active compounds, tested on confluent HeLa, Vero and peritoneal macrophage cell cultures, resulted in significantly higher selectivity indices (SI) than that of the reference drug benznidazole. Remarkably, several molecules of the tested panel strongly inhibited the parasite release from T. cruzi infected HeLa cell cultures suggesting an effect against the intracellular development of T. cruzi amastigotes as well. (C) 2013 Elsevier Ltd. All rights reserved.
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