Synthesis and in vitro antitubercular activity of ferrocene-based hydrazones

Bioorg Med Chem Lett. 2011 May 15;21(10):2866-8. doi: 10.1016/j.bmcl.2011.03.082. Epub 2011 Mar 30.

Abstract

We report here the synthesis and in vitro antitubercular activity of a new series of ferrocenyl derivatives. The quinoline-ferrocene hybrid 5 exhibited significant activity (MIC=2.5-5 μg/ml) against Mycobacterium tuberculosis. Results indicate that such hybrid compounds provide an efficient approach for future pharmacological developments to fight against tuberculosis. Moreover, the antimalarial drug candidate ferroquine (FQ, SSR97193) was also evaluated mainly because of its structural similarity. FQ was found to display moderate inhibitory activity (MIC=10-15 μg/ml) against M. tuberculosis. This new drug may offer an interesting alternative in endemic area where malaria and tuberculosis coexist.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology*
  • Ferrous Compounds / chemistry*
  • Hydrazones / chemical synthesis*
  • Hydrazones / chemistry
  • Hydrazones / pharmacology*
  • Metallocenes
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Mycobacterium tuberculosis / drug effects*

Substances

  • Antitubercular Agents
  • Ferrous Compounds
  • Hydrazones
  • Metallocenes
  • ferrocene