TABLE 1.
Inhibition of different bacterial Phe-RS enzymes by the phenyl-thiazolylurea-sulfonamides
| Enzyme and compound or drug | IC50 (μM)a
|
||
|---|---|---|---|
| E. coli | H. influenzaeb | S. pneumoniaeb | |
| Phe-RS | |||
| 1 | 0.007 | 0.02 | 0.2 |
| 2 | 0.008 | 0.008 | 0.2 |
| 3 | 0.015 | 0.015 | 0.3 |
| 4 | 0.015 | 0.015 | 0.05 |
| 5 | 0.025 | 0.06 | 0.04 |
| 6 | 0.02 | 0.02 | 0.2 |
| 7 | <0.005 | 0.01 | 0.3 |
| Ile-RS | |||
| Mupirocin | 0.0014b | 0.0014 | 0.0014 |
IC50s were determined for Phe-RS derived from different gram-negative and gram-positive pathogens. Inhibition of Ile-RS by mupirocin was measured in the presence of [14C]Ile instead of [14C]Phe; the results are included for comparison.
Values are the results of investigations performed using cell extracts.