Title
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
ISI
000294544900009
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.
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