Small azobenzene derivatives active against bacteria and fungi

Eur J Med Chem. 2013 Oct:68:178-84. doi: 10.1016/j.ejmech.2013.07.030. Epub 2013 Aug 11.

Abstract

ATP synthase and protein kinase (PKs) are prime targets for drug discovery in a variety of diseases. It is well known that numerous stilbenes are capable to interact and inhibit ATP synthase and PKs. This work focuses on a series of azobenzene based molecules having high structural similarity with antimicrobial stilbenes. An investigation was carried out analyzing the potential toxicity of a large set of molecules by means of computational analysis. A small selection of potential low toxic molecules have been therefore synthesized, characterized and finally microbiologically tested. The synthesized compounds show potent bactericidal activity against Gram+ and a fungus, and are capable of inhibiting biofilm formation. Finally, the compounds demonstrated a thermal stability that makes them potential candidates for incorporation in polymer matrix for application as biomedical devices and food packaging.

Keywords: ADMET; Antimicrobial; Azobenzenes.

MeSH terms

  • Anti-Infective Agents / chemistry*
  • Anti-Infective Agents / pharmacology*
  • Azo Compounds / chemistry*
  • Azo Compounds / pharmacology
  • Bacteria / drug effects*
  • Biofilms / drug effects
  • Computer Simulation*
  • Drug Discovery*
  • Fungi / drug effects*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Stilbenes / chemistry
  • Stilbenes / pharmacology
  • Structure-Activity Relationship

Substances

  • Anti-Infective Agents
  • Azo Compounds
  • Stilbenes
  • azobenzene