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Diarylquinolines, synthesis pathways and quantitative structure-activity relationship studies leading to the discovery of TMC207
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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. | | |
| Language |
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English
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| Source (journal) |
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Future medicinal chemistry | |
| Publication |
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2011
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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 (Publishers DOI) |
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