Table 3.
IC50 values for inhibition of RmlC by substituted triazinoindol-benzimidazolones, and the MIC values of these compounds against M. tuberculosis in culture.
 | ||||||
|---|---|---|---|---|---|---|
| Compound ID | R1 | R2 | n | Sulfone1 | IC50 (μM) | MIC (μg/ml)2 |
| 77074 | CH 2=CH-CH2 | H | 3 | No | 0.12 | 13 |
| SID 7975595 | CH3-CH2 | H | 3 | No | 0.2 | 19 |
| 77072 | CH3- | H | 3 | No | 0.5 | 9 |
| 77071 | CH3-CH2-CH2 | H | 3 | No | 1.25 | 9 |
| 77070 |  |
H | 3 | No | 2.9 | >50 |
| 77073 | H | H | 3 | No | 3.3 | ND |
| SID 7972845 | CH2=CH-CH2 | H | 1 | No | 10.3 | ND |
| 78531 | CH2=CH-CH2 | CH3 | 3 | No | 20 | 25 |
| 78532 | CH3-CH2 | H | 3 | Yes | 0.83 | ND |
| 78533 | CH2=CH-CH2 | H | 3 | Yes | 0.43 | ND |
1
Refers to oxidation of the thioether to a sulfone.
2
The MIC values were from at least 2 separate tests.
3
IC50 values markedly increased with time after compounds were dissolved in DMSO suggesting lack of stability.