Table 1. Antimycobacterial Activity Data of Newly Synthesized Compounds (4, 6d, 6g, 6i, and 6o) against Five Drug-Resistant Isolates of M. tuberculosis H37Rv.
| INH-R1a |
INH-R2b |
RIF-R1c |
RIF-R2d |
FQ-R1e |
|||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| compd | MIC (μM) | IC50 (μM) | IC90 (μM) | MIC (μM) | IC50 (μM) | IC90 (μM) | MIC (μM) | IC50 (μM) | IC90 (μM) | MIC (μM) | IC50 (μM) | IC90 (μM) | MIC (μM) | IC50 (μM) | IC90 (μM) |
| 4 | 5.3 | 1.3 | 6.6 | 2.5 | 0.79 | 2.9 | 4 | 1.1 | 4.6 | 4.8 | 1.2 | 5.9 | 17 | 2.8 | 16 |
| 6d | 15 | 12 | >50 | 12 | 8 | >50 | 25 | 11 | >50 | 31 | 8.7 | >50 | 22 | 23 | >50 |
| 6g | 24 | 12 | >200 | 13 | 7.1 | 12 | 28 | 9.2 | 27 | 46 | 19 | >200 | 30 | 18 | >200 |
| 6i | 32 | 9.1 | >25 | 19 | 5.6 | >25 | 17 | 7 | 19 | 41 | 10 | >25 | 33 | 13 | >25 |
| 6o | 3.2 | 0.68 | 3.8 | 1.5 | 0.38 | 1.7 | 2.2 | 0.54 | 2.6 | 6.3 | 0.76 | 9.2 | 21 | 2.3 | 33 |
| rifampicin | 0.018 | 0.0084 | 0.022 | 0.0065 | 0.0047 | 0.012 | 2 | 1.2 | 2.3 | >50 | >50 | >50 | 0.027 | 0.013 | 0.039 |
| isoniazid | >200 | >200 | >200 | >200 | >200 | >200 | 0.17 | 0.15 | 0.21 | 0.62 | 0.54 | 0.6 | 0.35 | 0.36 | 0.47 |
| levofloxacin | 1.2 | 0.64 | 1.4 | 1.4 | 0.84 | 1.4 | 0.76 | 0.59 | 0.91 | 1.1 | 0.6 | 1.2 | 20 | 12 | 22 |
a
INH-R1 was derived from H37Rv and is a katG mutant (Y155* = truncation).
b
INH-R2 is strain ATCC35822.
c
RIF-R1 was derived from H37Rv and is a nrpoB mutant (S522L).
d
RIF-R2 is strain ATCC35828.
e
FQ-R1 is a fluoroquinolone-resistant strain derived from H37Rv and is a gyrB mutant (D94N). INH, isoniazid; RIF, rifampicin; FQ, Fluoroquinolone.