Synthesis and evaluation of antimalarial activity of oxygenated 3-alkylpyridine marine alkaloid analogues

Chem Biol Drug Des. 2011 Sep;78(3):477-82. doi: 10.1111/j.1747-0285.2011.01154.x. Epub 2011 Jul 8.

Abstract

A series of new oxygenated analogues of marine 3-alkylpyridine alkaloids were prepared from 3-pyridinepropanol in few steps and in good yields. The key step for the synthesis of these compounds was a Williamson etherification under phase-transfer conditions. All new compounds were evaluated for their antiplasmodial activity and cytotoxicity. A significant reduction in parasitaemia was observed for some of the prepared compounds, and the majority of them exhibited a selectivity index (SI) ranging from 2.78 to 15.58, which suggests that these compounds may be a promising class of substances with antimalarial activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemical synthesis
  • Alkaloids / chemistry*
  • Alkaloids / pharmacology*
  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • Humans
  • Malaria, Falciparum / drug therapy*
  • Plasmodium falciparum / drug effects*
  • Pyridines / chemical synthesis
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Structure-Activity Relationship

Substances

  • Alkaloids
  • Antimalarials
  • Pyridines