Heteroaryl chalcones: design, synthesis, X-ray crystal structures and biological evaluation

Molecules. 2013 Oct 15;18(10):12707-24. doi: 10.3390/molecules181012707.

Abstract

Chalcone derivatives have attracted increasing attention due to their numerous pharmacological activities. Changes in their structures have displayed high degree of diversity that has proven to result in a broad spectrum of biological activities. The present study highlights the synthesis of some halogen substituted chalcones 3(a-i) containing the 5-chlorothiophene moiety, their X-ray crystal structures and the evaluation of possible biological activities such as antibacterial, antifungal and reducing power abilities. The results indicate the tested compounds show a varied range of inhibition values against all the tested microbial strains. Compound 3c with a p-fluoro substituent on the phenyl ring exhibits elevated antimicrobial activity, whereas the compounds 3e and 3f displayed the least antimicrobial activities. The compounds 3d, 3e, 3f and 3i showed good ferric and cupric reducing abilities, and the compounds 3b and 3c showed the weakest reducing power in the series.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / pharmacology
  • Antioxidants / chemical synthesis
  • Antioxidants / pharmacology
  • Chalcones / chemical synthesis*
  • Chalcones / pharmacology
  • Crystallography, X-Ray
  • Fusarium / drug effects
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Hydrogen Bonding
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Conformation
  • Reducing Agents / chemical synthesis
  • Reducing Agents / pharmacology
  • Thiophenes / chemical synthesis
  • Thiophenes / pharmacology

Substances

  • Anti-Bacterial Agents
  • Antifungal Agents
  • Antioxidants
  • Chalcones
  • Reducing Agents
  • Thiophenes