Diarylquinolines, Synthesis Pathways and Quantitative Structure–Activity Relationship Studies Leading to the Discovery of TMC207
Copyright policy )Diarylquinolines, Synthesis Pathways and Quantitative Structure–Activity Relationship Studies Leading to the Discovery of TMC207
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.
- Johnson & Johnson (United States) United States
- University of Antwerp Belgium
- Janssen-Cilag Spain
Models, Molecular, Molecular Structure, Cell Survival, Pharmacology. Therapy, Chemistry, Pharmaceutical, Mycobacterium smegmatis, Antitubercular Agents, Quantitative Structure-Activity Relationship, Microbial Sensitivity Tests, Mycobacterium tuberculosis, Chemistry, Drug Resistance, Multiple, Bacterial, Drug Discovery, Quinolines, Humans, Diarylquinolines, HeLa Cells
Models, Molecular, Molecular Structure, Cell Survival, Pharmacology. Therapy, Chemistry, Pharmaceutical, Mycobacterium smegmatis, Antitubercular Agents, Quantitative Structure-Activity Relationship, Microbial Sensitivity Tests, Mycobacterium tuberculosis, Chemistry, Drug Resistance, Multiple, Bacterial, Drug Discovery, Quinolines, Humans, Diarylquinolines, HeLa Cells
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