Table 4.
Designed 2-aminothiazol-4(5H)-one derivatives with 11β-HSD1 inhibitory activity predicted by the MLP 10-11-1 model
![]() | ||||
|---|---|---|---|---|
| Compound | R | R1 | R2 | Predicted log I11β‐HSD1 |
| 7b | ![]() |
H | CH3 | 1.3214 |
| 7c | H | C2H5 | 1.3654 | |
| 7d | H | n-C3H7 | 1.9376 | |
| 7e | H | CH(CH3)2 | 1.9213 | |
| 7f | CH3 | CH3 | 1.9128 | |
| 7 g | H | C6H5 | 1.8244 | |
| 7 h | H | p-BrC6H4 | 1.3436 | |
| 7i | C5H10cycl | 2.0133 | ||
| 7j | C3H6cycl | 1.9882 | ||
| 8a | ![]() |
H | H | 0.0000 |
| 8b | H | CH3 | 0.9940 | |
| 8c | H | C2H5 | 1.0459 | |
| 8d | H | n-C3H7 | 1.2294 | |
| 8e | H | CH(CH3)2 | 1.8577 | |
| 8f | CH3 | CH3 | 1.9598 | |
| 8 g | H | C6H5 | 1.1073 | |
| 8 h | H | p-BrC6H4 | 1.8062 | |
| 8i | C5H10cycl | 1.9745 | ||
| 8j | C3H6cycl | 1.2989 | ||
| 9a | ![]() |
H | H | 0.0000 |
| 9b | H | CH3 | 1.2529 | |
| 9c | H | C2H5 | 1.2989 | |
| 9d | H | n-C3H7 | 1.4561 | |
| 9e | H | CH(CH3)2 | 1.4561 | |
| 9f | CH3 | CH3 | 2.0031 | |
| 9 g | H | C6H5 | 1.3518 | |
| 9 h | H | p-BrC6H4 | 1.9668 | |
| 9i | C5H10cycl | 2.0226 | ||
| 9j | C3H6cycl | 1.9816 | ||
| 10a | ![]() |
H | H | 0.0000 |
| 10b | H | CH3 | 0.9889 | |
| 10c | H | C2H5 | 1.0366 | |
| 10d | H | n-C3H7 | 1.1541 | |
| 10e | H | CH(CH3)2 | 1.1541 | |
| 10f | CH3 | CH3 | 0.9889 | |
| 10 g | H | C6H5 | 0.7169 | |
| 10 h | H | p-BrC6H4 | 0.6904 | |
| 10i | C5H10cycl | 1.8769 | ||
| 10j | C3H6cycl | 1.7425 | ||




