Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2272-6. doi: 10.1016/j.bmcl.2008.03.009. Epub 2008 Mar 7.

Abstract

Taking advantage of the structural features of natural products showing anti-trypanosomatid activity, we designed and synthesized a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives. The library was obtained following a parallel approach and using readily available synthons. All the derivatives showed inhibitory activity toward either Trypanosoma or Leishmania species, with 8, 10, and 16 being the most active compounds against Trypanosoma brucei rhodesiense, Leishmania donovani, and Trypanosoma cruzi cells (IC(50)=50nM, IC(50)=0.28microM, and IC(50)=1.26microM, respectively).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anthraquinones / chemical synthesis
  • Anthraquinones / pharmacology*
  • Antiprotozoal Agents / chemical synthesis
  • Antiprotozoal Agents / pharmacology*
  • Drug Design*
  • Inhibitory Concentration 50
  • Leishmania / drug effects*
  • Models, Chemical
  • Naphthoquinones / chemical synthesis
  • Naphthoquinones / pharmacology*
  • Parasitic Sensitivity Tests
  • Trypanosoma / drug effects*

Substances

  • Anthraquinones
  • Antiprotozoal Agents
  • Naphthoquinones