Table 1.
Antibacterial activities of the most active CyC analogsa.
Compounds | Extracellular growth | Intracellular macrophage growthb | ||
---|---|---|---|---|
MIC50 (µM) | MIC50 (µM) | CC50 (µM) | ||
Isoniazid (INH)c | 1.2 | 1.2 | >150 | |
Ethionamide (ETO)c | 6.0 | 6.0 | 120 | |
Rifampicin (RIF)c | 0.01 | 2.9 | 24 | |
CyC 6(β) |
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No effect | 12.6 | >100 |
CyC 7(α) |
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92.6 | 4.5 | >100 |
CyC 7(β) | 16.6 | 3.1 | >100 | |
CyC 8(α) |
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40.4 | 4.0 | >100 |
CyC 8(β) | >100 | 11.7 | >20 | |
CyC 17 |
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0.50 | No effect | >100 |
CyC 18(α) |
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24.4 | No effect | >100 |
CyC 18(β) | 1.7 | No effect | >100 |
aExperiments were performed as described in Materials and Methods. MIC50: compound minimal concentration leading to 50% growth inhibition. CC50: compound concentration leading to 50% host cell toxicity. The best MIC50 obtained are highlighted in bold. Values are means of three independent assays performed in triplicate (CV% < 5%). bRaw264.7 macrophages were infected by M. tb H37Rv-GFP at a MOI of 2. cData from20.