Table 1.
Chemical modification of methyl acarviosin. (a) α-Glucosidase inhibitory activity of several anhydro, deoxy, and O-methyl derivatives. (b) α-Glucosidase inhibitory activity of several 1,4-anhydro derivatives 116a–h.
| (a) | |
|---|---|
| Compd | Inhibitory activity |
| (IC50, µM) α-Glucosidase (Baker’s yeast) | |
| 70 | 0.98 |
| 77 | 0.38 |
| 102a | 1.25 |
| b | 0.75 |
| 104 | 1.45 |
| (b) | ||||
|---|---|---|---|---|
| Compd | Inhibitory activity | |||
| (IC50, µM) α-Glucosidase (Baker’s yeast) | ||||
|
| ||||
| X | Y | Z | ||
| 116a | OH | H | OH | 0.10 |
| b | N3 | H | OH | 0.29 |
| c | NH2 | H | OH | 2.2 |
| d | NHAc | H | OH | 33 |
| e | F | H | OH | 0.18 |
| f | H | OH | OH | 0.50 |
| g | H | H | OH | 0.032 |
| h | H | H | H | 0.030 |