Table 1.
Phosphotransferase Enzyme Inhibitory Activities of Capuramycin Analogues.a
| Entry | Compound | IC50 (μM)a | |||
|---|---|---|---|---|---|
| MraY (Hydrogenivirga sp.) | WecA (E. coli) | AglH (M. jannaschii) | DPAGT1 (Human) | ||
| 1 | Capuramycin (CAP, 1) | 0.13 | >50 | >50 | >50 |
| 2 | O-Methyl capuramycin (OM-CAP, 2) | >50 | 0.060 | 2.5 | 4.5 |
| 3 | iso-Capuramycin (I-CAP, 3) | 8.5 | 30.0 | 20.0 | 11.5 |
| 4 | Demethyl capuramycin (DM-CAP, 4) | >50 | 35.0 | >50 | >50 |
| 5 | Capuramycin phenoxypiperidinylbenzylamide (CPPB, 5) | 10.3 | 0.10 | 0.15 | 0.20 |
| 6 | iso-Capuramycin phenoxypiperidinylbenzylamide (I-CPPB, 6) | >50 | 20.0 | 15.0 | 0.60 |
| 7 | O-Methyl capuramycin phenoxypiperidinylbenzylamide (OM-CPPB, 7) | 5.0 | 10.0 | 30.0 | 20.0 |
| 8 | Demethyl capuramycin phenoxypiperidinylbenzylamide (DM-CPPB, 8) | >50 | 30.0 | >50 | >50 |
| 9 | Capuramycin phenoxypiperidinylbenzylamine (CPPA, 9) | >50 | >50 | >50 | >50 |
| 10 | iso-Capuramycin phenoxypiperidinylbenzylamine (I-CPPA, 10) | >50 | >50 | >50 | >50 |
| 11 | Tunicamycin (11) | 2.9 | 0.15 | 13.2 | 1.5 |
a
All assay protocols are summarized in Experimental Section as well as SI.