Table 3.
In vitro activities of select triclosan derivatives against M. tuberculosis InhA.[a]
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|---|---|---|---|
| Cmpd | R1 | R2 | InhA IC50 (nM) |
| 8 | CH2CH3 | Cl | 120 ± 19 |
| 9 | (CH2)2CH3 | Cl | 91 ± 15 |
| 10 | (CH2)3CH3 | Cl | 55 ± 20 |
| 11 | CH2CH(CH3)2 | Cl | 96 ± 46 |
| 12 | (CH2)2CH(CH3)2 | Cl | 63 ± 9 |
| 13 | CH2CH(CH3)CH2CH3 | Cl | 130 ± 56 |
| 14 | 2-pyridyl | CN | >10000 |
| 15 | 3-pyridyl | Cl | >10000 |
| 16 | 4-pyridyl | CN | >10000 |
| 17 | CH2(2-pyridyl) | Cl | 29 ± 11 |
| 18 | CH2(3-pyridyl) | Cl | 42 ± 10 |
| 19 | CH2(4-pyridyl) | CN | 75 ± 16 |
| 20 | o-CH3-Ph | Cl | 1300 ± 77 |
| 21 | o-CH3-Ph | CN | >10000 |
| 22 | m-CH3-Ph | Cl | 870 ± 110 |
| 23 | p-F-Ph | Cl | >10000 |
| 24 | CH2Ph | Cl | 51 ± 6 |
| 25 | (CH2)2Ph | Cl | 21 ± 8 |
| 26 | (CH2)3Ph | Cl | 50 ± 14 |
Values reported as the mean ± standard error for at least three independent measurements.
