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Newlands Press, Future Medicinal Chemistry, 11(3), p. 1345-1360, 2011

DOI: 10.4155/fmc.11.79

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Diarylquinolines, synthesis pathways and quantitative structure–activity relationship studies leading to the discovery of TMC207

Journal article published in 2011 by Jerome Guillemont, Christophe Meyer ORCID, Alain Poncelet, Xavier Bourdrez, Koen Andries
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

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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.