3-(1,3,4-Thiadiazole-2-yl)quinoline derivatives: synthesis, characterization and anti-microbial activity

Eur J Med Chem. 2011 Jul;46(7):3158-66. doi: 10.1016/j.ejmech.2011.04.013. Epub 2011 Apr 13.

Abstract

A new series of thiadiazoles and intermediate thiosemicarbazones were synthesized from the chloroquinone molecule, with an aim to explore their effect on in vitro growth of microorganisms causing microbial infection. The chemical structures of the compound were elucidated by elemental analysis, FTIR, 1H and 13C NMR and ESI-MS spectral data. In vitro anti-microbial activity was performed against Staphylococcusaureus, Streptococcuspyogenes, Salmonellatyphimurium, and Escherichiacoli. The MIC was detected using the double dilution method. The results were compared by calculating percent inhibit area/μg of the compounds and the standard "amoxicillin". The selected compounds were tested for cytotoxic results using MTT assay H9c2 cardiac myoblasts cell line and the results showed that all the compounds offered remarkable >80% viability to a concentration of 200 μg/mL.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Cell Line
  • Cell Survival / drug effects
  • Escherichia coli / drug effects
  • Escherichia coli / growth & development
  • Hydroxyquinolines / chemical synthesis*
  • Hydroxyquinolines / pharmacology
  • Microbial Sensitivity Tests
  • Myocytes, Cardiac / cytology
  • Myocytes, Cardiac / drug effects
  • Rats
  • Salmonella typhimurium / drug effects
  • Salmonella typhimurium / growth & development
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / growth & development
  • Streptococcus pyogenes / drug effects
  • Streptococcus pyogenes / growth & development
  • Thiadiazoles / chemical synthesis*
  • Thiadiazoles / pharmacology
  • Thiosemicarbazones / chemical synthesis*
  • Thiosemicarbazones / pharmacology

Substances

  • Anti-Bacterial Agents
  • Hydroxyquinolines
  • Thiadiazoles
  • Thiosemicarbazones