Effectiveness of novel 5-(5-amino-1-aryl-1H-pyrazol-4-yl)-1H-tetrazole derivatives against promastigotes and amastigotes of Leishmania amazonensis

Chem Biol Drug Des. 2014 Mar;83(3):272-7. doi: 10.1111/cbdd.12235. Epub 2013 Oct 30.

Abstract

In this research, a series of substituted 5-(5-amino-1-aryl-1H-pyrazol-4-yl)-1H-tetrazoles were synthesized and evaluated for in vitro antileishmanial activity. Among the derivatives, examined compounds 3b and 3l exhibited promising activity against promastigotes and amastigotes forms of Leishmania amazonensis. The cytotoxicity of these compounds was evaluated on murine cells, giving access to the corresponding selectivity index (SI).

Keywords: Leishmania amazonensis; antileishmanial activity; tetrazole derivatives.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemical synthesis
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • Leishmania / drug effects*
  • Mice
  • Mice, Inbred BALB C
  • Tetrazoles / chemical synthesis
  • Tetrazoles / chemistry*
  • Tetrazoles / pharmacology*

Substances

  • Antiprotozoal Agents
  • Tetrazoles