Table 2. Pleuromutilins with Other Boron Heterocycles Linked via C(14).
| ID | P | Q–R | R8 | Wolbachia infected C6/36 cells (wAlb) EC50 (nM) | Wolbachia infected LDW1 cells (wMel) EC50 (nM) |
|---|---|---|---|---|---|
| 40 | CH3SO2N | N=CH | H | 9 | 0.8 |
| 41 | CH3N | N=CH | H | 14.8 | 1.5 |
| 42 | CH3C(=O)N | N=CH | H | 4 | 0.2 |
| 43 | Boc-N | N=CH | H | 0.7 | 0.2 |
| 44 | HN | N=CH | H | 3.5 | 2.7 |
| 45 | CH3OC(=O)N | N=CH | H | 1.5 | 0.3 |
| 46 | O | N=CH | H | 14.2 | 5.1 |
| 47 | CH3SO2N | N=CH | 8-F | 240 | 6.3 |
| 48 | CH3N | N=CH | 8-F | 172 | 11 |
| 49 | CH3C(=O)N | N=CH | 8-F | 107 | NTa |
| 50 | CH3OC(=O)N | N=CH | 8-F | 164 | 1.3 |
| 51 | O | N=CH | 8-F | 329 | 27 |
| 52 | CH3C(=O)N | N=CH | 8-CH3 | 26.1 | NT |
| 53 | O | CH2CH2 | H | >1000 | NT |
NT = not tested.
