Table 1.
Assays against a library of capuramycin analogues against the WecA enzyme (P-60 from E. coli B21WecA).
 | |||||
|---|---|---|---|---|---|
| entry | Compound | WecA inhibition (%)a | IC50 (µg/mL)b | ||
| 0.02 µg/mL | 2 µg/mL | 20 µg/mL | |||
| 1 | Tunicamycin (5) | 36.0 (38.5)c | 97.0 (100) | 100 (100) | 0.120 ± 7.80 |
| 2 | Capuramycin (6) | - | - | - | - |
| 3 | UT-01309 (7) | - | - | - | - |
| 4 | SQ641 (8) | - | - | - | - |
| 5 | UT-03347 (9) | 11.0 (15.5) | 23.0 (29.0) | 80.5 (84.5) | ND |
| 6 | UT-03328 (10) | 0 (0) | 23.0 (28.0) | 60.5 (75.5) | ND |
| 7 | UT-03325 (11) | 30.0 (35.0) | 35.0 (45.0) | 55.0 (60.5) | ND |
| 8 | UT-01320 (12) | 42.0 (45.0) | 100 (100) | 100 (100) | 0.0354 ± 9.14 |
| 9 | DMSO | 0 (0) | 0 (0) | 0 (0) | - |
a
1) Reaction conditions: UDP-Glucosamine-C6-FITC (1, 0.56 µL), MgCl2 (0.5 M; 4 µL); CHAPS (5%; 10 µl), β-mercaptoethanol (50 mM, 5µL) Tris-buffer (pH = 8.0; 50 mM, 9.74 µL), C50-P (4mM, 1.7 µL), P-60 (E. coli B21WecA) (18 µL), 37 °C, 2h.; The Km :194.7 µM (for 1).
b
Each experiment was performed three times, and the average IC50 values were summarized.
c
WecA inhibitory activity in parentheses were obtained via HPLC.