Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

Bioorg Med Chem. 2009 Aug 15;17(16):6063-72. doi: 10.1016/j.bmc.2009.06.051. Epub 2009 Jun 27.

Abstract

A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25microg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry*
  • Antitubercular Agents / pharmacology
  • Cell Line
  • Chlorocebus aethiops
  • Hydrazones / chemical synthesis
  • Hydrazones / chemistry*
  • Hydrazones / pharmacology
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects
  • Structure-Activity Relationship
  • Vero Cells

Substances

  • Antitubercular Agents
  • Hydrazones