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Title
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Diarylquinolines, synthesis pathways and quantitative structure-activity relationship studies leading to the discovery of TMC207
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Author
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Abstract
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| 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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Language
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English
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Source (journal)
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Future Medicinal Chemistry. - London, 2009, currens
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Publication
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London
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Future Science Ltd
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2011
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ISSN
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1756-8927
1756-8919
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Volume/pages
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3
:11
(2011)
, p. 1345-1360
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ISI
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000294544900009
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Full text (Publisher's DOI)
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