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Table 1 Anticonvulsant activity of the new compounds 8a–m in PTZ and MES tests

From: Hybridization of the effective pharmacophores for treatment of epilepsy: design, synthesis, in vivo anticonvulsant activity, and in silico studies of phenoxyphenyl-1,3,4-oxadiazole-thio-N-phenylacetamid hybrids

Compound

Dose (mg/kg)

PTZa

MESb

Number of animals protected / Number of tested animals

%Protection

Number of animals protected / Number of tested animals

%Protection

8a

1

–

–

5/8

62.5

 

2

–

–

2/4

50

 

5

0/4

0

2/4

50

 

10

–

–

2/4

50

 

20

–

–

2/4

50

8b

1

–

–

0/4

0

 

10

–

–

1/4

25

 

50

0/4

0

4/10

40

 

100

–

–

3/4

75

8c

1

–

–

0/4

0

 

2

0/4

0

1/4

25

 

5

–

–

1/4

25

 

10

–

–

1/4

25

 

20

–

–

3/4

75

8d

1

–

–

1/4

25

 

2

–

–

2/4

50

 

5

0/4

0

2/4

50

 

10

–

–

2/4

50

 

20

–

–

1/4

25

8e

1

–

–

1/4

25

 

5

0/4

0

1/4

25

 

10

–

–

1/4

25

8f

5

0/4

0

0/4

0

 

10

–

–

1/4

25

 

20

–

–

3/4

75

8g

1

–

–

5/8

62.5

 

2

–

–

2/8

25

 

5

0/4

0

2/4

50

 

10

–

–

3/4

75

 

20

–

–

5/8

62.5

8h

1

–

–

0/4

0

 

2

–

–

1/4

25

 

5

0/4

0

1/4

25

 

10

–

–

1/4

25

 

20

–

–

2/4

50

8i

1

–

–

0/4

0

 

5

0/4

0

2/4

50

 

10

–

–

1/4

25

 

20

–

–

2/4

50

8j

1

–

–

1/4

25

 

5

0/4

0

2/4

50

 

10

1/4

25

2/4

50

8k

2

0/4

0

3/4

75

 

5

–

–

3/4

75

 

10

–

–

2/4

50

8k c

2

–

–

0/4

0

8L

1

–

–

1/4

25

 

2

0/4

0

1/4

25

 

5

1/4

25

3/4

75

 

10

0/4

0

2/4

50

8m

1

0/4

0

1/4

25

 

2

–

–

2/4

50

 

10

–

–

0/8

0

 

50

–

–

0/4

0

Diazepam

2

6/6

100

6/6

100

Diazepamc

2

0/6

0

0/6

0

  1. aPentylentetrazole (100 mg/kg, ip) induced lethal convulsion
  2. bMaximal electroshock seizure test: 50 mA, 60 Hz, ac, 0.2 s
  3. cFlumazenil as a selective benzodiazepine receptor antagonist (1 mg/kg, ip) was administered 15 min before seizure induction
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BMC Chemistry

ISSN: 2661-801X

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