Table 2. Structures and Activity of N-Benzylated Analogues against MTB H37Rv.
| compd. | n1 | n2 | R | LogP | MIC (μM) |
|---|---|---|---|---|---|
| 11c | 1 | 1 | H | 5.78 | 0.847 |
| 11j | 1 | 1 | 4-methoxyl | 5.91 | 1.005 |
| 11k | 1 | 1 | 4-fluoro | 5.92 | 0.210 |
| 11l | 1 | 1 | 4-bromo | 6.67 | 0.057 |
| 11m | 1 | 1 | 4-trifluoromethyl | 6.76 | <0.035 |
| 11n | 1 | 1 | 3-fluoro | 5.92 | 0.054 |
| 11o | 1 | 1 | 3,5-difluoro | 6.06 | <0.035 |
| 11p | 1 | 1 | 3,5-dimethoxyl | 6.05 | 0.825 |
| 12c | 0 | 1 | H | 5.33 | 0.059 |
| 12e | 0 | 1 | 4-methoxyl | 5.46 | 0.112 |
| 12f | 0 | 1 | 4-fluoro | 5.46 | <0.035 |
| 12g | 0 | 1 | 2-methoxyl | 5.46 | 1.676 |
| 13d | 0 | 0 | 4-methoxyl | 5.00 | 0.113 |
| PBTZ 169 | <0.035 |