title: Aromatic glycosyl disulfide derivatives: evaluation of their inhibitory activities against Trypanosoma cruzi.
abstract: Aromatic oligovalent glycosyl disulfides and some diglycosyl disulfides were tested against three different Trypanosoma cruzi strains. Di-(β-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 μM at 37 °C. The inhibitory activities were maintained, although somewhat lowered, at a temperature of 4 °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.
authors: Department of Medical Technology, Faculty of Health Sciences, University of Antofagasta, P.O. Box 170, Antofagasta, Chile.
authors: Bessy
authors: B
authors: Gutiérrez
authors: Christian
authors: C
authors: Muñoz
authors: Luis
authors: L
authors: Osorio
authors: Krisztina
authors: K
authors: Fehér
authors: Tünde-Zita
authors: TZ
authors: Illyés
authors: Zsuzsa
authors: Z
authors: Papp
authors: Ambati Ashok
authors: AA
authors: Kumar
authors: Katalin E
authors: KE
authors: Kövér
authors: Hernán
authors: H
authors: Sagua
authors: Jorge E
authors: JE
authors: Araya
authors: Patricio
authors: P
authors: Morales
authors: László
authors: L
authors: Szilágyi
authors: Jorge
authors: J
authors: González
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D001555:Benzene Derivatives / Q000494:pharmacology; D014355:Chagas Disease / Q000188:drug therapy; D002522:Chlorocebus aethiops; D004220:Disulfides / Q000737:chemistry / Q000494:pharmacology*; D006027:Glycosides / Q000737:chemistry / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development; D014709:Vero Cells
chemical_list: D000981:Antiprotozoal Agents; D001555:Benzene Derivatives; D004220:Disulfides; D006027:Glycosides