Synthesis of new chalcone derivatives containing a rhodanine-3-acetic acid moiety with potential anti-bacterial activity

Eur J Med Chem. 2010 Dec;45(12):5739-43. doi: 10.1016/j.ejmech.2010.09.031. Epub 2010 Sep 19.

Abstract

With an intention to synergize the anti-bacterial activity of chalcones and rhodanine-3-acetic acid, several hybrid compounds possessing chalcone and rhodanine-3-acetic acid moieties were synthesized and tested for their anti-bacterial activity. Some compounds presented great anti-microbial activities against Gram-positive bacteria (including the multidrug-resistant clinical isolates). This class of compounds presented high potency against Staphylococcus aureus, among which the derivatives 5k with a MIC of 2 μg/mL was as active as the standard drug (norfloxacin) and less active than oxacillin. Compounds 5a-s did not inhibit the growth of Gram-negative bacteria Escherichia coli CCARM 1924 or E. coli CCARM 1356 at 64 μg/mL.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Chalcone / chemical synthesis*
  • Chalcone / chemistry
  • Chalcone / pharmacology*
  • Dose-Response Relationship, Drug
  • Escherichia coli / drug effects
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Rhodanine / analogs & derivatives
  • Rhodanine / chemistry*
  • Staphylococcus / drug effects*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Chalcone
  • Rhodanine