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Trypanosoma cruzi: activities of lapachol and alpha- and beta-lapachone derivatives against epimastigote and trypomastigote forms.

Bioorganic & medicinal chemistry (2007-11-22)
Cristian Salas, Ricardo A Tapia, Karina Ciudad, Verónica Armstrong, Myriam Orellana, Ulrike Kemmerling, Jorge Ferreira, Juan Diego Maya, Antonio Morello
ABSTRACT

Derivatives of natural quinones with biological activities, such as lapachol, alpha- and beta-lapachones, have been synthesized and their trypanocidal activity evaluated in vitro in Trypanosoma cruzi cells. All tested compounds inhibited epimastigote growth and trypomastigote viability. Several compounds showed similar or higher activity as compared with current trypanocidal drugs, nifurtimox and benznidazole. The results presented here show that the anti-T. cruzi activity of the alpha-lapachone derivatives can be increased by the replacement of the benzene ring by a pyridine moiety. Free radical production and consequently oxidative stress through redox cycling or production of electrophilic metabolites are the potential biological mechanism of action for these synthetic quinones.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Lapachol, 98%

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