Characterization of Two Novel Inhibitors of the Mycobacterium tuberculosis Cytochrome bc1 Complex

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY(2023)

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摘要
Drug-resistant tuberculosis is a global health care threat calling for novel effective treatment options. Here, we report on two novel cytochrome bc(1) inhibitors (MJ-22 and B6) targeting the Mycobacterium tuberculosis respiratory chain with excellent intracellular activities in human macrophages. Both hit compounds revealed very low mutation frequencies and distinct cross-resistance patterns with other advanced cytochrome bc(1) inhibitors. Drug-resistant tuberculosis is a global health care threat calling for novel effective treatment options. Here, we report on two novel cytochrome bc(1) inhibitors (MJ-22 and B6) targeting the Mycobacterium tuberculosis respiratory chain with excellent intracellular activities in human macrophages. Both hit compounds revealed very low mutation frequencies and distinct cross-resistance patterns with other advanced cytochrome bc(1) inhibitors.
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关键词
Mycobacterium tuberculosis, QcrB, antibiotic, cytochrome bc(1), ATP, drug screening
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