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  • Title: Diarylquinolines, synthesis pathways and quantitative structure--activity relationship studies leading to the discovery of TMC207.
    Author: Guillemont J, Meyer C, Poncelet A, Bourdrez X, Andries K.
    Journal: Future Med Chem; 2011 Sep; 3(11):1345-60. PubMed ID: 21879841.
    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.
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