Table 1.
Phase-I evaluation of anticonvulsant activity in mice (i.p.).
| Compound | R | MES a | Toxicity | ||
|---|---|---|---|---|---|
| 100 | 30 | 100 | 30 | ||
| 4a | –CH3 | 0/3 | - b | 0/3 | - |
| 4b | –H | 0/3 | - | 0/3 | - |
| 4c | n-C5H11 | 2/3 | 0/3 | 0/3 | - |
| 4d | n-C6H13 | 3/3 | 0/3 | 0/3 | - |
| 4e | n-C7H15 | 3/3 | 1/3 | 0/3 | - |
| 4f | n-C8H17 | 1/3 | - | 0/3 | - |
| 4g | n-C9H19 | 0/3 | - | 0/3 | - |
| 4h | n-C10H21 | 0/3 | - | 0/3 | - |
| 4i | –CH2C6H5 | 2/3 | 0/3 | 0/3 | - |
| 4j | –CH2C6H4 (o-F) | 2/3 | 0/3 | 1/3 | - |
| 4k | –CH2C6H4 (m-F) | 2/3 | 0/3 | 0/3 | - |
| 4l | –CH2C6H4 (p-F) | 1/3 | - | 0/3 | - |
| 4m | –CH2C6H4 (o-Cl) | 2/3 | 0/3 | 0/3 | - |
| 4n | –CH2C6H4 (m-Cl) | 2/3 | 0/3 | 1/3 | - |
| 4o | –CH2C6H4 (p-Cl) | 0/3 | 0/3 | 1/3 | - |
| 4p | –CH2C6H3 (2,4-2Cl) | 0/3 | 0/3 | 0/3 | - |
| 4q | –CH2C6H3 (2,6-2Cl) | 2/3 | - | 2/3 | 0/3 |
| 4r | –CH2C6H4 (m-CF3) | 0/3 | - | 0/3 | - |
| 4s | –CH2C6H4 (p-CH3) | 1/3 | - | 0/3 | - |
| 4t | –CH2C6H4 (o-CN) | 0/3 | - | 0/3 | - |
| 9a | n-C6H13 | 3/3 | 1/3 | 0/3 | - |
| 9b | n-C7H15 | 1/3 | - | 0/3 | - |
| 9c | n-C8H17 | 0/3 | - | 0/3 | - |
| 9d | –CH2C6H5 | 2/3 | 1/3 | 0/3 | - |
| 9e | –CH2C6H4 (p-Cl) | 0/3 | - | 0/3 | - |
a Maximal electroshock test (number of animals protected/number of animals tested), the number of mice is three; The dose measured in mg/kg; b Not tested.