Synthetic approaches towards bedaquiline and its derivatives

Bioorg Med Chem Lett. 2020 Jun 15;30(12):127172. doi: 10.1016/j.bmcl.2020.127172. Epub 2020 Apr 7.


Bedaquiline is a diarylquinoline drug that demonstrates potent and selective inhibition of mycobacterial ATP synthase, and is clinically administered for the treatment of multi-drug resistant tuberculosis. Due to its excellent activity and novel mechanism of action, bedaquiline has been the focus of a number of synthetic studies. This review will discuss these synthetic approaches, as well as the synthesis and bioactivity of the numerous derivatives and molecular probes inspired by bedaquiline.

Keywords: Bedaquiline; Diarylquinolines; SAR; Stereoselective synthesis; Tuberculosis.

Publication types

  • Review

MeSH terms

  • Alkynes / chemistry
  • Animals
  • Antitubercular Agents / chemical synthesis*
  • Azides / chemistry
  • Catalysis
  • Cycloaddition Reaction
  • Diarylquinolines / chemical synthesis*
  • Drug Evaluation, Preclinical
  • Humans
  • Molecular Structure
  • Mycobacterium tuberculosis / drug effects*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Triazoles / chemistry
  • Tuberculosis, Multidrug-Resistant / drug therapy*


  • Alkynes
  • Antitubercular Agents
  • Azides
  • Diarylquinolines
  • Triazoles
  • bedaquiline