Table 4. Antimycobacterial Profiles of Indolecarboxamide 16 and Indolylmethylamine 33.
M. bovis BCG (μM) |
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M. tb H37Rv (μM) |
MIC50/MIC90 in 7H9 media |
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no. | MIC50a | MIC90a | MBC99.9b | MBC99.9b | standard media | no glycerol | with 10% FBS | Vero IC50 (μM)c |
16 | 0.02 | 0.04 | 0.08 | 0.08 | 0.02/0.04 | 0.01/d | 0.02/0.08 | >100 |
33 | 0.05 | 0.13 | 0.63 | 0.16 | 0.04/0.08 | 0.04/d | 0.07/0.16 | 22 ± 2 |
Lowest concentration required to reduce bacterial growth by 50% (MIC50) or 90% (MIC90) compared to untreated cultures. MIC50 and MIC90 of isoniazid (control) on M. tb were 1.8 μM and 3.8 μM.
Minimum compound concentration required to kill 99.9% of bacteria. Control isoniazid had MBC99Mtb of 3.2 μM and MBC99.9BCG of 10 μM.
Concentration required to reduce growth of mammalian Vero cells by 50% compared to untreated controls. Selectivity indices (IC50Vero/MIC50, SIs) for 16 was >5000 (M. tb, M. bovis BCG), and for 33, SI was 366 (M. tb) and 550 (M. bovis BCG).
MIC90 could not be accurately determined in 7H9 in the absence of glycerol due to poor bacterial growth.