Synthesis, antimicrobial activity, and QSAR studies of furan-3-carboxamides

Bioorg Med Chem. 2007 Mar 1;15(5):1947-58. doi: 10.1016/j.bmc.2007.01.003. Epub 2007 Jan 4.

Abstract

The synthesis and characterization of a new series of furan-3-carboxamides, from the aromatization of 4-trichloroacetyl-2,3-dihydrofuran to 3-trichloroacetyl furan followed by nucleophilic displacement of the trichloromethyl group or the corresponding carboxylic acid chloride by nitrogen-containing compounds, is presented. Preliminary in vitro antimicrobial activity of the title compounds was assessed against a panel of microorganisms including yeast, filamentous fungi, bacteria, and alga. Some of the furan-3-carboxamides exhibited significant in vitro antimicrobial activity. QSAR investigation was applied to find a correlation between the different physicochemical parameters of the compounds studied and their biological activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis*
  • Amides / chemistry
  • Amides / pharmacology*
  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Fungi / classification
  • Fungi / drug effects
  • Furans / chemistry*
  • Magnetic Resonance Spectroscopy
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Quantitative Structure-Activity Relationship
  • Spectrometry, Mass, Electrospray Ionization

Substances

  • Amides
  • Antifungal Agents
  • Furans