Table 3. 2,4-Dichloroaniline substitutions. Compounds were tested for activity against M. tuberculosis (MBC4.5) and HepG2 cells (IC50). MBC4.5 are reported as the median. HepG2 IC50 are reported as the mean ± standard deviation. The number of replicates is in parentheses.
| ||||
Cpd | ID | R1 | MBC4.5 (μM) | HepG2 IC50 (μM) |
16 | IDR-0600849 | BuNH- | 100 (4) | 59 ± 0.71 (2) |
17 | IDR-0597328 | Cyclopropyl-NH- | >200 (2) | >100 (2) |
18 | IDR-0600848 | Propargyl-NH- | >200 (5) | 83 ± 12 (2) |
19 | IDR-0600851 | Cycloheptyl-NH- | >200 (5) | 24 ± 6.4 (2) |
20 | IDR-0600850 | 2-Adamantyl-NH- | >200 (4) | 20 ± 4.2 (2) |
21 | IDR-0600833 | Piperidyl- | >200 (2) | >100 (5) |
22 | IDR-0600834 | Morpholinyl- | >200 (2) | >100 (5) |
23 | IDR-0600866 | 4-Me-Piperazinyl- | >200 (4) | >100 (2) |
24 | IDR-0597331 | 2-Pyridyl-NH- | 113 (6) | 52 ± 13 (2) |
25 | IDR-0597270 | 2,4-Cl–Ph–NMe- | >200 (2) | 60 ± 9.9 (2) |