Table 1.
Compound | R1 | R2 | MIC H37Rv (μM) | Vero CC50 (μM) | MLM t1/2 (min) | Kinetic Aqueous Solubility (μM) |
---|---|---|---|---|---|---|
DG167a | 0.39 | 23 | 10.1 | 324 | ||
4 | H | NHSO2-n-Bu | 1.6 | >190 | nd | nd |
5 | CO2Et | NHSO2-n-Bu | 0.20 | >150 | <0.5 | 0.895 |
8 | CONH2 | NHSO2-n-Bu | 3.1 | >160 | 6.16 | 45.5 |
9 | CN | NHSO2-n-Bu | 0.78 | 170 | 6.51 | 133 |
10 | CN | NHSO2-n-Pen | 0.20 | 160 | 4.08 | 7.21 |
11 | CH2NH2 | NHSO2-n-Bu | 100 | 170 | nd | nd |
nd, not determined.
Kumar et al. (2018) reference.