Table 1.
Phase I anticonvulsant screening of the compounds in micea
|
Comp.
No. |
R |
MES
b
|
PTZ
b
|
NT
b
|
miLogP | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 30b | 100 | 300 | 30 | 100 | 300 | 30 | 100 | 300 | - | ||
| 3a | H | - | 1/3c | 3/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 3/3 | 2.1 |
| 3b | 2-F | - | 1/3 | 2/3 | - | 0/3 | 0/3 | 0/3 | 1/3 | 3/3 | 2.2 |
| 3c | 4-F | 1/3 | 3/3 | 3/3 | - | 0/3 | 0/3 | 0/3 | 2/3 | 3/3 | 2.3 |
| 3d | 2-Cl | - | 0/3 | 1/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 1/3 | 2.8 |
| 3e | 3-Cl | - | 0/3 | 0/3 | - | 1/3 | 2/3 | 0/3 | 0/3 | 0/3 | 2.8 |
| 3f | 4-Cl | - | 0/3 | 0/3 | - | 0/3 | 1/3 | 0/3 | 0/3 | 0/3 | 2.8 |
| 3g | 2-Br | - | 0/3 | 0/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 0/3 | 2.9 |
| 3h | 3-Br | - | 0/3 | 1/3 | - | 0/3 | 2/3 | 0/3 | 0/3 | 1/3 | 2.9 |
| 3i | 4-Br | - | 0/3 | 3/3 | 0/3 | 2/3 | 3/3 | 0/3 | 1/3 | 3/3 | 2.9 |
| 3j | 4-NO2 | - | 0/3 | 2/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 2/3 | 2.1 |
| 3k | 4-CH3 | - | 1/3 | 3/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 2/3 | 2.6 |
| 3l | 4-OCH3 | - | 1/3 | 3/3 | - | 1/3 | 2/3 | 0/3 | 1/3 | 3/3 | 2.2 |
| 5a | C2H5 | - | 0/3 | 1/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 1/3 | 2.6 |
| 5b | C3H7 | 0/3 | 2/3 | 3/3 | 1/3 | 3/3 | 3/3 | 0/3 | 2/3 | 3/3 | 3.1 |
| 5c | C4H9 | - | 1/3 | 3/3 | - | 1/3 | 2/3 | 0/3 | 2/3 | 3/3 | 3.6 |
| 5d | C5H11 | - | 0/3 | 2/3 | - | 0/3 | 0/3 | 0/3 | 1/3 | 3/3 | 4.1 |
| 5e | C7H15 | - | 0/3 | 0/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 0/3 | 5.1 |
| 5f | CH2C6H5 | - | 0/3 | 0/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 0/3 | 3.8 |
| 5g | CH2C6H5(2-F) | - | 0/3 | 0/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 0/3 | 3.9 |
| 5h | CH2C6H5(3-F) | - | 0/3 | 0/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 0/3 | 3.9 |
| 5i | CH2C6H5(4-F) | - | 0/3 | 0/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 0/3 | 4.0 |
| 5j | CH2C6H5(2-Cl) | - | 0/3 | 0/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 0/3 | 4.4 |
| 5k | CH2C6H5(3-Cl) | - | 0/3 | 0/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 0/3 | 4.4 |
| 5l | CH2C6H5(4-Cl) | - | 0/3 | 0/3 | - | 0/3 | 0/3 | 0/3 | 0/3 | 0/3 | 4.5 |
All positive reaction numbers are in bold italic.
a
: Animals was administered intraperitoneal injection.
b
: Doses of 30, 100 and 300 mg/Kg were administered in maximal electroshock seizure test (MES), pentylenetetrazole-induced seizure test (PTZ), and neurotoxicity (NT) tests.
c
: The figures n/n indicate the number of animals protected/number of animals tested. The number of mice used is three. Sign “-” in the table means not tested.