Table 3.
Biological Evaluation of Extended-Reach Azithromycin Analogsa
| Linker | Indole | IC50 | MIC50 | |
|---|---|---|---|---|
| 119 | C3H8 |
|
0.54 | 0.78 |
| 120 | C3H8 |
|
0.88 | 0.78 |
| 121 | C3H8 |
|
0.227 | 1.56 |
| 122 | C3H8 |
|
0.128 | 1.56 |
| 123 | C3H8 |
|
0.49 | 0.78 |
| 124 | C3H8 |
|
0.147 | 1.56 |
| 125 | C6H4 |
|
0.12 | 3.13 |
| 126 | C6H4 |
|
0.197 | 1.56 |
| azithromycin (36) | 0.292 | 0.78 |
IC50 values in μM and tested against cell-free E. coli ribosomes; MIC50 values in μg/mL against a susceptible strain of S. aureus; green denotes an increased activity; orange, decreased; yellow, equipotent.