Table 2. Effects of imidazo[1,2-a]pyridine-N-glycinyl-hydrazone derivatives 1a–k on TNF-α production and cell viability in murine peritoneal macrophages.
| Compound | TNF-α a | % of cell viability b | SelectivityIndex(SI) d | cLog P e | ||
| % inhibition at 10 µM | IC50(µM)c | at 10 µM | IC50 (µM)c(0.1–100) | |||
| 1a | 95.3* | 0.62 (0.03–10) | 20.1* | 6.9 | 11.1 | 4.2 |
| 1b | 77.3* | 0.34 (0.03–30) | 78.4 | 14.7 | 43.2 | 4.2 |
| 1c | 18.3 | – | 100 | – | – | 3.2 |
| 1d | 56.7* | 3.67 (0.1–30) | 100 | – | – | 3.3 |
| 1e | 53.8* | 3.05 (0.1–30) | 100 | – | – | 4.3 |
| 1f | 29.3 | – | 100 | – | – | 3.7 |
| 1g | 5.6 | – | 100 | – | – | 3.8 |
| 1h | 2.8 | – | 100 | – | – | 3.2 |
| 1i | 78.0* | 0.21 (0.03–30) | 73.3 | 21.7 | 103.3 | 4.3 |
| 1j | 90.8* | 0.31 (0.03–10) | 40.0* | 10.4 | 33.5 | 4.3 |
| 1k | 75.8* | 0.99 (0.03–30) | 83.2 | 23.5 | 23.7 | 4.7 |
| SB-203580 | 90.0* | 0.22 (0.03–10) | 44.3* | 9.7 | 44.0 | – |
| LASSBio-1504 (2) | 96.9* | 3.60 (0.1–30) | 61.5* | 10.3 | 2.8 | 6.0 |
The results are expressed as the apercent inhibition and bpercent cell viability compared to the vehicle (DMSO); n = 3 independent experiments performed in duplicate;
*p = 0.05 using student’s t test; cIC50 values were determined using at least five concentrations, the range concentration are showed in parentheses; d SI = cytotoxicity IC50/anti-TNF-α IC50; e values calculated using ACDLABS software.