Antiproliferative and ultrastructural effects of phenethylamine derivatives on promastigotes and amastigotes of Leishmania (Leishmania) infantum chagasi

Parasitol Int. 2017 Apr;66(2):47-55. doi: 10.1016/j.parint.2016.11.010. Epub 2016 Nov 22.

Abstract

Leishmania (Leishmania) infantum chagasi is one of the agents that cause visceral leishmaniasis. This disease occurs more frequently in third world countries, such as Brazil. The treatment is arduous, and is dependent on just a few drugs like the antimonial derivatives and amphotericin B. Moreover, these drugs are not only expensive, but they can also cause severe side effects and require long-term treatment. Therefore, it is very important to find new compounds that are effective against leishmaniasis. In the present work we evaluated a new group of synthetic amides against the promastigote and amastigote forms of L. infantum chagasi. The results showed that one of these amides in particular, presented very effective activity against the promastigotes and amastigotes of L. infantum chagasi at low concentrations and it also presented low toxicity for mammal cells, which makes this synthetic amide a promising drug for combating leishmaniasis.

Keywords: Cellular damage; L. chagasi; Phenethylamine.

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemical synthesis
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Brazil
  • Cell Line
  • Drug Discovery
  • Leishmania / drug effects
  • Leishmania / ultrastructure
  • Leishmania infantum / drug effects*
  • Leishmania infantum / growth & development
  • Leishmania infantum / physiology
  • Leishmania infantum / ultrastructure
  • Life Cycle Stages / drug effects
  • Macrophages, Peritoneal / drug effects
  • Mice
  • Phenethylamines / chemical synthesis
  • Phenethylamines / chemistry
  • Phenethylamines / pharmacology*

Substances

  • Antiprotozoal Agents
  • Phenethylamines