A new chemotype with promise against Trypanosoma cruzi

Bioorg Med Chem Lett. 2020 Jan 1;30(1):126778. doi: 10.1016/j.bmcl.2019.126778. Epub 2019 Oct 31.


Pyridyl benzamide 2 is a potent inhibitor of Trypanosoma cruzi, but not other protozoan parasites, and had a selectivity-index of ≥10. The initial structure-activity relationship (SAR) indicates that benzamide and sulfonamide functional groups, and N-methylpiperazine and sterically unhindered 3-pyridyl substructures are required for high activity against T. cruzi. Compound 2 and its active analogs had low to moderate metabolic stabilities in human and mouse liver microsomes.

Keywords: Chagas disease; SAR; Trypanosoma cruzi.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Chagas Disease / drug therapy*
  • Humans
  • Structure-Activity Relationship
  • Trypanocidal Agents / pharmacology
  • Trypanocidal Agents / therapeutic use*
  • Trypanosoma cruzi / drug effects*


  • Trypanocidal Agents