Antitrypanosomal and antioxidant properties of 4-hydroxycoumarins derivatives

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5569-73. doi: 10.1016/j.bmcl.2012.07.013. Epub 2012 Jul 13.

Abstract

In the present communication we prepared a series of six 4-hydroxycoumarin derivatives, isosters of quercetin, recognized as an antioxidant natural compound, with the aim of evaluating the antitrypanosomal activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, and the antioxidant properties. We have used the 4-hydroxycoumarin moiety (compound 1) as the molecular template for the synthesis of compounds 2-7. These derivates have shown moderate trypanocidal activity. However they have been proved to be good antioxidants. In particular compound 7 is the most active antioxidant and it is, therefore, a potential candidate for a successful employment in conditions characterized by free radicals overproduction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 4-Hydroxycoumarins / chemistry*
  • 4-Hydroxycoumarins / pharmacology*
  • Antioxidants / chemistry*
  • Antioxidants / pharmacology*
  • Chagas Disease / drug therapy
  • Humans
  • Structure-Activity Relationship
  • Trypanocidal Agents / chemistry*
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma cruzi / drug effects*

Substances

  • 4-Hydroxycoumarins
  • Antioxidants
  • Trypanocidal Agents