Table 3.
Structures and biological activity of 8-substituted tetrahydronaphthalenes.
| No | R3 | Yielda |
MIC90b (μg/mL) |
IC50c (μg/mL) |
clogPd | |
|---|---|---|---|---|---|---|
| % | MABA | LORA | VERO | |||
| 5 |  |
55 | 0.8 | 1.5 | 11 | 6.76 |
| 62 |  |
100 | 1.0 | 1.5 | 11 | 5.76 |
| 63 |  |
86 | 0.90 | 0.91 | 10 | 7.18 |
| 64 |  |
78 | 1.9 | 1.2 | 13 | 6.77 |
| 65 |  |
63 | 0.74 | 1.2 | 5.8 | 6.51 |
| 66 |  |
82 | 0.93 | 1.7 | 9.9 | 6.96 |
| 67 |  |
84 | >32 | >32 | >32 | 7.15 |
| 68 |  |
92 | >32 | >32 | >32 | 5.77 |
| 69 |  |
32 | >32 | >32 | >32 | 6.97 |
| 70 |  |
85 | >32 | >32 | >32 | 8.37 |
| 71 |  |
88 | 1.9 | >32 | >32 | 6.70 |
| 72 |  |
62 | 3.7 | 4.3 | >32 | 6.70 |
| 73 |  |
80 | 29 | >32 | >32 | 7.52 |
| 74 |  |
63 | >32 | >32 | >32 | 7.42 |
| 75 |  |
22 | >32 | >32 | >32 | 6.70 |
| 76 |  |
53 | 15 | >32 | >32 | 4.94 |
| 77 |  |
82 | 4.0 | 5.4 | >32 | 6.51 |
| 78 |  |
10 | 15 | 14 | >32 | 6.53 |
| 79 |  |
74 | 7.7 | >32 | >32 | 6.32 |
