In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor

Antimicrob Agents Chemother. 2007 Nov;51(11):4202-4. doi: 10.1128/AAC.00181-07. Epub 2007 Aug 20.

Abstract

The diarylquinoline R207910 is in clinical development for tuberculosis treatment. The MIC(50) for 41 drug-susceptible and 44 multidrug-resistant Mycobacterium tuberculosis clinical isolates was 0.032 microg/ml. Out of 20 additional mycobacterial species, three were found to be naturally resistant to R207910 and were shown to exhibit a polymorphism in their atpE genes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Synthetase Complexes / antagonists & inhibitors*
  • ATP Synthetase Complexes / genetics
  • ATP Synthetase Complexes / metabolism
  • Amino Acid Sequence
  • Antitubercular Agents / pharmacology*
  • Diarylquinolines
  • Drug Resistance, Bacterial
  • Microbial Sensitivity Tests
  • Molecular Sequence Data
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / enzymology
  • Mycobacterium tuberculosis / genetics
  • Polymorphism, Genetic
  • Quinolines / pharmacology*
  • Sequence Homology, Amino Acid

Substances

  • Antitubercular Agents
  • Diarylquinolines
  • Quinolines
  • bedaquiline
  • ATP Synthetase Complexes