4-Diazopyrazole derivatives as potential new antibiofilm agents

Chemotherapy. 2008;54(6):456-62. doi: 10.1159/000159271. Epub 2008 Oct 1.

Abstract

Background: The recognition that chronic infections and infections associated with medical devices are biofilm related has been the impulse for investigating the antibiofilm properties of some diazopyrazoles biologically active as antimicrobials.

Methods: The susceptibility of staphylococcal biofilms was determined at concentrations ranging from 25 to 1.5 microg/ml using crystal violet and methylthiazotetrazolium (MTT) staining. In the case of Candida albicans, we first assessed the anti-germ tube formation effect of 4-NO2 (compound 1c) and then we evaluated its antibiofilm activity at concentrations ranging from 100 to 6.2 microg/ml.

Results: All the compounds were active against reference staphylococcal biofilm strains at the maximum tested concentration of 25 microg/ml; despite its remarkable activity as germ tube inhibitor, compound 1c showed weak activity against C. albicans biofilms at 100 microg/ml.

Conclusion: 4-Diazopyrazoles represent an interesting source of antimicrobial compounds in the development of new antibiofilm agents.

MeSH terms

  • Aza Compounds / chemistry
  • Aza Compounds / pharmacology*
  • Biofilms / drug effects*
  • Candida albicans / drug effects
  • Candida albicans / physiology
  • Molecular Structure
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*
  • Staphylococcus / drug effects

Substances

  • Aza Compounds
  • Pyrazoles