Table 2.
Inhibition of TG activity and the antibacterial determinations of selected hits
| Compound* | IC50, μM† | MIC, μM‡ |
|||
|---|---|---|---|---|---|
| B. subtilis (ATCC23857) | E. faecalis (ATCC29212) | S. aureus (ATCC29213) | S. pneumoniae (ATCC49619) | ||
| 1 | 0.36 | 0.33 | 0.04 | <0.01 | 0.33 |
| 2 | 2.10 | 2.50 | 10.0 | 1.25 | 20.0 |
| 4 | 0.92 | 1.25 | 5.0 | 0.625 | 20.0 |
| 5 | 125.00 | — | — | — | — |
| 6 | 34.00 | 0.25 | 0.25 | 1.0 | 4.0 |
| 7 | 3.70 | 0.25 | 1.0 | 4.0 | — |
| 8 | 9.30 | 4.0 | >4.0 | >4.0 | >4.0 |
*Compounds 2, 4, and 5 are moenomycin derivatives. Compounds 6–8 were HTS hits.
†IC50 values were determined by using the fluorescence anisotropy assay shown in Fig. 5A.
‡The MICs of moenomycin against different bacterial species were determined as described in Materials and Methods. ATCC, American Type Culture Collection.