Thiopurine derivatives containing triazole and steroid: synthesis, antimalarial and antileishmanial activities

Biomed Pharmacother. 2011 Jun;65(3):198-203. doi: 10.1016/j.biopha.2010.10.013. Epub 2010 Nov 5.

Abstract

A series of novel 6-thiopurine derivates containing 1,2,3-triazole were synthesized and their in vivo antimalarial activity and in vitro antileishmanial activity were examined. The compounds 10, 11, 12 and 14 presented higher values of inhibition of parasite multiplication than chloroquine. For antileishmanial activity, the compound 14 showed activity against the three species of Leishmania tested. None of compounds showed cytotoxicity against mammalian cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetic Acid / chemistry
  • Animals
  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology
  • Antiprotozoal Agents / chemical synthesis
  • Antiprotozoal Agents / chemistry*
  • Antiprotozoal Agents / pharmacology
  • Chloroquine / chemistry
  • Female
  • Leishmania / drug effects*
  • Mercaptopurine / analogs & derivatives*
  • Mercaptopurine / chemical synthesis
  • Mercaptopurine / chemistry
  • Mercaptopurine / pharmacology
  • Mice
  • Plasmodium / drug effects*
  • Steroids / chemical synthesis
  • Steroids / chemistry
  • Steroids / pharmacology*
  • Triazoles / chemical synthesis
  • Triazoles / chemistry
  • Triazoles / pharmacology*

Substances

  • Antimalarials
  • Antiprotozoal Agents
  • Steroids
  • Triazoles
  • Chloroquine
  • Mercaptopurine
  • Acetic Acid