Table 2.
PK inhibitory activity and antimicrobial activity of compounds 22a–g
| |||||
|---|---|---|---|---|---|
| Analogs | IC50a (nM) | MICb (μg/ml) | X | Y | Substitutions |
| 10a | 21.4 | 2.0 | |||
| 22a | 151.7 | >64 | S | N | 6-Bromo |
| 22b | 107.6 (2) | >64 | O | CH | 6-Bromo |
| 22c | 14.0 | >64 | S | CH | 6-Bromo |
| 22d | 358.1 | >64 | S | N | 5-Bromo |
| 22e | 45% @ 10 μM | ND | O | CH | 5-Bromo |
| 22f | 42% @ 1 μM | >64 | S | CH | 5-Bromo |
| 22g | 4.1 | >64 | S | N | 5,6′-Dibromo |
a
IC50 values are calculated from a triplicate 15-point titration or are an average of (n) such determinations as indicated. Alternatively the % inhibition at the highest concentration tested is presented.
b
Minimum concentration to give >98% inhibition of growth of S. aureus ATCC 29213 (single determination). Control MIC (vancomycin) is 1 μg/ml.