Antiparasitic activities of novel pyrimidine N-acylhydrazone hybrids

Drug Dev Res. 2021 Apr;82(2):230-240. doi: 10.1002/ddr.21745. Epub 2020 Sep 30.

Abstract

In this article, a series of 29 new pyrimidine N-acylhydrazone hybrids were synthesized and evaluated in vitro against Leishmania amazonensis and Trypanosoma cruzi protozoa that cause the neglected diseases cutaneous leishmaniasis and Chagas disease, respectively. Eight of the target compounds showed significant antiprotozoal activities with IC50 values in 4.3-33.6 μM range. The more active compound 4f exhibited selectivity index greater than 15 and drug-like properties based on Lipinski's rule.

Keywords: Chagas disease; Leishmania amazonensis; N-acylhydrazone; Trypanosoma cruzi; leishmaniasis; pyrimidine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiparasitic Agents / chemistry
  • Antiparasitic Agents / pharmacology*
  • Humans
  • Hydrazones / chemistry
  • Hydrazones / pharmacology*
  • Leishmania braziliensis / drug effects*
  • Leishmania braziliensis / physiology
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Trypanosoma cruzi / drug effects*
  • Trypanosoma cruzi / physiology

Substances

  • Antiparasitic Agents
  • Hydrazones
  • Pyrimidines
  • pyrimidine