Table 2 Biological data of the first series of triazole analogs 14a-l and 23-26
From: Targeting bacterial kinases as a strategy to counteract antibiotic resistance
Entry | Structure | R | ΔTm (°C) at 500 µM | Inhibition (%) at 10 µM | Ki (nM) | X-ray structure resolution (Å) |
14a | -H | 1.31 | 83% | 1,300 ± 55 | 2.30 | |
14b |
| 1.12 | 77% | 2,400 ± 320 | 2.06 | |
14c |
| 1.20 | 88% | 458 ± 37 | ND | |
14 d |
| 1.36 | 24% | 14,500 ± 1,400 | ND | |
23 |
| 1.48 | 91% | 425 ± 32 | 2.30 | |
14e |
| 2.04 | 82% | 2,400 ± 160 | ND | |
24 |
| 0.45 | 82% | 799 ± 81 | 2.45 | |
25 |
| -0.20 | 62% | 9,900 ± 600 | ND | |
26 |
|
| -0.33 | 25% | >10,000 | ND |
14 f |
| 0.49 | 87% | 916 ± 78 | 2.50 | |
14 g |
| -0.20 | 40% | >10,000 | ND | |
14 h |
| 0.23 | 73% | 6,300 ± 1,000 | ND | |
14i |
| 0.16 | 72% | 2,700 ± 450 | ND | |
14j |
| 1.03 | 84% | 376 ± 21 | ND | |
14k |
| 0.37 | 63% | 6,500 ± 400 | 2.55 | |
14 l |
| 0.26 | 44% | 16,200 ± 3,700 | ND |
