Please use this identifier to cite or link to this item:
Type
ArticleCopyright
Restricted access
Collections
- IOC - Artigos de Periódicos [12967]
Metadata
Show full item record
SYNTHESIS AND ANTI-TRYPANOSOMA CRUZI ACTIVITY OF NEW 3-PHENYLTHIO-NOR-B-LAPACHONE DERIVATIVES
Author
Affilliation
Abstract
We report herein a straightforward and efficient one-step reaction to prepare new nor-b-lapachone
derivatives tethered with phenylthio groups at position 3 of the furan ring. We have screened the compounds
on bloodstream trypomastigotes of Trypanosoma cruzi, the causative agent of Chagas disease,
aimed at finding a new prototype with high trypanocidal activity. The new compounds possess a broad
range of activity (IC50/24 h from 9.2 to 182.7 lM), higher than the original quinone (391.5 lM) and four of
them higher than standard drug benznidazole (103.6 lM). The most active was compound 13b (9.2 lM),
being 11 times active than benznidazole and the less toxic derivative to heart muscle cells.
Share