Table 2.
Antitubercular activities of saturated acid and ester MEPicides
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|---|---|---|---|---|
| Cmpd No. | R1 | R2 | R3 |
M. tuberculosis MIC (µg/mL)* |
| INH | N/A | N/A | N/A | 0.01 |
| 1 (Fos) | H | H | H/Na | >500 |
| 2 (FR900098) | H | CH3 | H/Na | >500 |
| 3 | H | CH3 | CH2OCOtBu | 50–100 (62.5) |
| 8e | H | Ph | H/Na | ≥200 |
| 8h | H | (CH2)3Ph | H/Na | >200 |
| 7h | H | (CH2)3Ph | CH2CH3 | 200 |
| 12 | H | (CH2)3Ph | CH2OCOtBu | 150 |
| 8d | H | (CH2)2cyclohexyl | H/Na | >200 (25) |
| 7d | H | (CH2)2cyclohexyl | CH2CH3 | >200 (37) |
| 8l | H | CH2O(4-Cl)Ph | H/Na | >200 (25) |
| 16d | (4-ipr)Bn | CH3 | H/Na | 200 (25) |
| 17 | (4-ipr)Bn | CH3 | CH2OCOtBu | 12.5 (6.25–12.5) |
| 16k | CH2-4-(1,1’-biphenyl) | CH3 | H/Na | 25–50 |
| 15k | CH2-4-(1,1’-biphenyl) | CH3 | CH2CH3 | 200 (100) |
| 19 | CH2-4-(1,1’-biphenyl) | CH3 | CH2OCOtBu | 12.5 (3.13–6.25) |
| 16p | CH2-4-(4’-ipr)-1,1’-biphenyl | CH3 | H/Na | 100 (6.25–12.5) |
| 16h | (CH2)4Ph | CH3 | H/Na | ≥200 |
| 15h | (CH2)4Ph | CH3 | CH2CH3 | 100–200 |
| 21 | (CH2)4Ph | CH3 | CH2OCOPh | 25 |
| 18 | (CH2)4Ph | CH3 | CH2OCOtBu | 12.5 (6.25–12.5) |
| 16j | CH2-(2-naphthyl) | CH3 | H/Na | ≥200 |
| 15j | CH2-(2-naphthyl) | CH3 | CH2CH3 | 200 (100) |
| 20 | CH2-(2-naphthyl) | CH3 | CH2OCOtBu | 18.75 (4.7) |
Data using 7H9 media. When different, MIC in GAST-Fe media is given in parentheses.
