- Journal
- FUTURE MEDICINAL CHEMISTRY
- Année
- 2011
- Volume
- 3
- Numéro
- 11, SI
- Pages
- 1345-1360
- Mois
- SEP
- DOI
- 10.4155/FMC.11.79
Abstract
The emergence of multidrug-resistant strains of Mycobacterium tuberculosis and resistance to current anti-TB drugs call for the discovery and development of new effective anti-TB drugs. TMC207 is the lead candidate of a novel class of antimycobacterial agents, the diarylquinolines, which specifically inhibit mycobacterial ATP synthase and displays high activity against both drug-susceptible and multidrug-resistant strains of Mycobacterium tuberculosis. This article covers both synthesis pathways as well as qualitative and quantitative analyses of the structure-activity relationships of the diarylquinoline series on Mycobacterium smegmatis activity.