In vitro and in vivo assessment of newer quinoxaline-oxadiazole hybrids as antimicrobial and antiprotozoal agents

Int J Antimicrob Agents. 2017 Sep;50(3):413-418. doi: 10.1016/j.ijantimicag.2017.04.016. Epub 2017 Jul 4.

Abstract

A new series of N-(substituted-phenyl)-2-[5-(quinoxalin-2-yloxymethyl)-[1,3,4] oxadiazol-2-ylsulfanyl]-acetamides (5a-o) was designed and synthesised from the parent compound 2-hydroxy quinoxaline (1) through a multistep reaction sequence and was characterised by spectral and elemental analyses. All of the compounds synthesised were evaluated for their antimicrobial and antiprotozoal activities. The results revealed that quinoxaline-based 1,3,4-oxadiazoles displayed promising antibacterial, antifungal and anti-Trypanosoma cruzi activities compared with reference drugs, particularly the lead compound 5l in a short-term in vivo model in T. cruzi.

Keywords: 1,3,4-Oxadiazole; Antimicrobial; Antiprotozoal; Quinoxaline.

MeSH terms

  • Animals
  • Anti-Infective Agents / administration & dosage*
  • Anti-Infective Agents / pharmacology*
  • Bacteria / drug effects
  • Chagas Disease / drug therapy
  • Disease Models, Animal
  • Fungi / drug effects
  • Male
  • Mice
  • Molecular Structure
  • Oxadiazoles / administration & dosage*
  • Oxadiazoles / chemical synthesis
  • Oxadiazoles / chemistry
  • Oxadiazoles / pharmacology*
  • Quinoxalines / administration & dosage*
  • Quinoxalines / chemical synthesis
  • Quinoxalines / chemistry
  • Quinoxalines / pharmacology*
  • Trypanosoma cruzi / drug effects*

Substances

  • Anti-Infective Agents
  • Oxadiazoles
  • Quinoxalines