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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gutiérrez B,Muñoz C,Osorio L,Fehér K,Illyés TZ,Papp Z,Kumar AA,Kövér KE,Sagua H,Araya JE,Morales P,Szilágyi L,González J

doi

10.1016/j.bmcl.2013.04.030

subject

Has Abstract

pub_date

2013-06-15 00:00:00

pages

3576-9

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00511-8

journal_volume

23

pub_type

信件

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