Title
Diarylquinolines, synthesis pathways and quantitative structure-activity relationship studies leading to the discovery of TMC207 Diarylquinolines, synthesis pathways and quantitative structure-activity relationship studies leading to the discovery of TMC207
Author
Faculty/Department
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
Subject
Chemistry
Pharmacology. Therapy
Source (journal)
Future medicinal chemistry
Volume/pages
3(2011) :11 , p. 1345-1360
ISSN
1756-8919
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
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 structureactivity relationships of the diarylquinoline series on Mycobacterium smegmatis activity.
Handle