Table 1.
Inhibitory activity against replicating Mtb and mammalian cell toxicity of compounds.
| Compound identification | Compound name | Other identifier | Log P | MIC (µM) in supplemented media | Inhibition and selectivity (Vero cell line) | ||||
|---|---|---|---|---|---|---|---|---|---|
| 7H9 OADC |
7H9 ADC | 7H9 CAS | GAST/Fe | Cyto-toxicity IC50 (µM) | SI (IC50/MIC) | ||||
| 127-09 | N-[(E)-1-[(5-oxo-2-thioxo-imidazolidin-4-yl)methyl]hexylideneamino]pyridine-4-carboxamide | Pyridine carboxamide analogue | 2.18 | 1.6–3.1 | 1.6 | 0.4 | 0.4 | – | – |
| 127-17 | N-[(E)-(5-isopropenyl-2-methyl-cyclohex-2-en-1-ylidene)amino]pyridine-3-carboxamide | Pyridine carboxamide analogue |
2.94 | 1.6–3.1 | 6.3 | 1.6 | 1.0 | 420 | 280 |
| 127-21 | N-[1,1,4-trioxo-2-[4-(trifluoromethyl)phenyl]-1,3-thiazolidin-3-yl]pyridine-4-carboxamide | Pyridine carboxamide analogue | 1.72 | 1.6–3.1 | 6.3 | 1.6 | 0.5 | > 160 | > 25.4 |
| 127-23 | N-[(E)-[2-hydroxy-1-(6-nitro-3-oxo-4H-quinoxalin-2-yl)-2-(4-nitrophenyl)ethylidene]amino]pyridine-4-carboxamide | Pyridine carboxamide analogue | 3.74 | 3.1–6.3 | 12.5 | 3.1 | 3.1 | > 130 | > 10.4 |
| 127-11 | [amino-(3,4-dichlorobenzoyl)-methoxy-methyl-dioxo-yl]methyl carbamate | Mitomycin derivative T 56 | 1.03 | 0.4 | 0.1 | 0.8 | < 0.2 | 3.75 | 62.5 |
| 127-13 | benzyl N-[(E)-[(2E)-2-(carbamothioylhydrazono)propylidene]amino]carbamodithioate | 3.42 | 1.6–3.1 | 1.6 | 1.6 | 25 | 38.4 | 64 | |
| 127-14 | 2-[2-[(E)-[2-(5H-benzo[a]phenazin-7-yl)-4-oxo-1-naphthylidene]amino]anilino]naphthalene-1,4-dione | 5.45 | 12.5 | 6.3 | 6.3 | 6.3 | 98.5 | 15.6 | |
| 127-15 | 10H-3,10a-Epidithiopyrazino[1,2-a]indole-1,4-dione, 2,3-dihydro-2,3,10,10-tetramethyl- | 4.00 | 0.4–0.8 | 0.1 | 0.4 | < 0.2 | 19 | 31.6 | |
| 127-18 | 2,7-dimethyl-[1,4]benzodioxino[2,3-f][4,7]phenanthroline-4,5-diol | 2.81 | 12.5 | 25 | 25 | 1.4 | 163 | 6.52 | |
| 127-19 | 7-methyl-3-nitroso-2-phenyl-imidazo[1,2-a]pyridine | 3.11 | 0.8–1.6 | 0.7 | 0.1 | < 0.2 | 52.7 | 33 | |
| 127-20 | N1,N4-bis[4-(1-methylimidazo[1,2-a]pyridin-1-ium-2-yl)phenyl]terephthalamide | 5.80 | 1.6 | 1.4 | – | < 0.2 | > 4300 | > 3071 | |
| 127-22 | N,N’-bis[5-[[5-[(3-amino-3-imino-propyl)carbamoyl]-1-methyl-pyrrol-3-yl]carbamoyl]-1-methyl-pyrrol-3-yl]decanediamide | −2.06 | 3.1 | 1.6 | 12.5 | < 0.2 | 54.22 | 100 | |
| MN-6925 | [(E)-dibenzofuran-2-ylmethyleneamino]thiourea | 2.69 | 6.3–12.5 | 3.1 | 6.3 | 3.1 | 74 | > 23.9 | |
| MN-9483 | Naphtho[1’,2’:4,5]imidazo[1,2-a]pyridine-5,6-dione | 1.71 | 3.1 | 1.6 | 3.1 | 0.4 | > 252 | > 158 | |
Is not determined.