Pyrimido[1,2-a]quinoxaline 6-oxide and phenazine 5,10-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi

Eur J Med Chem. 2008 Aug;43(8):1737-41. doi: 10.1016/j.ejmech.2007.10.031. Epub 2007 Nov 4.

Abstract

Two different families of N-oxide containing heterocycles were evaluated as in vitro growth inhibitors of T. cruzi. Both families of heterocycles were selected from our in-house library of compounds as analogues of active anti-T. cruzi N-oxide containing heterocycles. Derivatives from pyrimido[1,2-a]quinoxaline 6-oxide family were poorly active at the assayed doses. However, phenazine 5,10-dioxide derivatives displayed good to excellent anti-T. cruzi activities. The anti-T. cruzi activity of phenazine derivatives was related to substituent' electronic descriptors, sigma(p)(-). Derivatives 19, 20 and 23 were the most cytotoxic compounds against the protozoan and became excellent hit for further structural modifications.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Cyclic N-Oxides / chemical synthesis*
  • Cyclic N-Oxides / chemistry
  • Cyclic N-Oxides / pharmacology*
  • Electrons
  • Inhibitory Concentration 50
  • Molecular Structure
  • Phenazines / chemical synthesis*
  • Phenazines / chemistry
  • Phenazines / pharmacology*
  • Quinoxalines / chemical synthesis*
  • Quinoxalines / chemistry
  • Quinoxalines / pharmacology*
  • Structure-Activity Relationship
  • Trypanosoma cruzi / cytology
  • Trypanosoma cruzi / drug effects*

Substances

  • Antimalarials
  • Cyclic N-Oxides
  • Phenazines
  • Quinoxalines