Synthesis and characterization of some new quinoline based derivatives endowed with broad spectrum antimicrobial potency

Bioorg Med Chem Lett. 2012 Nov 15;22(22):6871-5. doi: 10.1016/j.bmcl.2012.09.039. Epub 2012 Sep 21.

Abstract

The synthesis of a novel series of 2-(5-(2-chloro-6-fluoroquinolin-3-yl)-3-(aryl)-4,5-dihydro-1H-pyrazol-1-yl)thiazol-4(5H)-ones (4a-l) and N-(4-(2-chloro-6-fluoroquinolin-3-yl)-6-(aryl)pyrimidin-2-yl)-2-morpholinoacetamides (7a-l) are described in the present paper. The chemical structures of compounds have been elucidated by IR, (1)H NMR, (13)C NMR and mass spectral data. Antimicrobial activity was measured against Escherichia coli (MTCC 443), Pseudomonas aeruginosa (MTCC 1688), Staphylococcus aureus (MTCC 96), Streptococcus pyogenes (MTCC 442), Candida albicans (MTCC 227), Aspergillus niger (MTCC 282) and Aspergillus clavatus (MTCC 1323) by serial broth dilution. Evaluation of antimicrobial activity showed that several compounds exhibited greater activity than reference drugs and thus could be promising new lead molecules.

MeSH terms

  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology
  • Fungi / drug effects
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Microbial Sensitivity Tests
  • Molecular Conformation
  • Quinolines / chemical synthesis
  • Quinolines / chemistry*
  • Quinolines / pharmacology
  • Structure-Activity Relationship
  • Thiazoles / chemistry

Substances

  • Anti-Infective Agents
  • Quinolines
  • Thiazoles
  • quinoline