Table 4.
Antinociceptive Activity of Compounds 7a–r in Mouse WWTW Assaya
| C-8 substitution | antinociceptive activity at 10 mg/kg | duration of action | C-8 substitution | antinociceptive activity at 10 mg/kg | duration of action | ||
|---|---|---|---|---|---|---|---|
| 7a | benzyl | no activity | 7j | methylmorpholine | no activity | ||
| 7b | methyl | fully efficacious | 1.5 h | 7k | methylpiperazine | did not test | |
| 7c | ethyl | fully efficacious | 1.0 h | 7l | phenethyl | no activity | |
| 7d | n-propyl | no activity | 7m | ethyl amide | no activity | ||
| 7e | n-butyl | fully efficacious | 2.5 h | 7n | ethyl ester | fully efficacious | 2.5 h |
| 7f | t-butyl | partially active | 7o | phenyl amide | did not test | ||
| 7g | fluoro | no activity | 7p | benzyl amide | no activity | ||
| 7h | trifluoromethyl | no activity | 7q | bromo | no activity | ||
| 7i | methylpiperidine | no activity | 7r | carboxylic acid | no activity |
Results from the mouse WWTW assay after ip administration of compound 7a–r at 10 mg/kg. Antinociceptive activities defined as fully efficacious for 20 s latency to tail withdrawal, partially active for 10 s above baseline, or no activity for no significant difference from baseline. Duration of action is defined here as the time it takes to return to baseline after a 10 mg/kg bolus injection of test compound.