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. Author manuscript; available in PMC: 2011 Feb 11.
Published in final edited form as: J Med Chem. 2010 Feb 11;53(3):1288. doi: 10.1021/jm901563p

Table 4.

Evaluation of Selected (R)-N-(4-Substituted)benzyl 2-Acetamido-3-methoxypropionamide Derivatives in the Rat Hippocampal Kindled Seizure Model Assaya

graphic file with name nihms168020u8.jpg
Preliminary Hippocampal Kindling Test (Rat)
Hippocampal Kindled Rat (0.25 h) (ip)
Seizure Score
After discharge duration (sec)

No. R4 Pre-drug Drug Pre-drug Drug ED50 (mg/kg) (interval)
(R)-17 CH2OCH3 5 0 40 – 69 12 87 (58 – 129)
(R)-20 (CH2)3OCH3 4 – 5 2 21 – 40 21 ND
(R)-21 CH=CH2 4 – 5 0 27 – 43 0–11 ND
(R)-34 N3 4 0 29 – 65 0 6 (3 – 9)
(R)-36 Cl 4 – 5 0 25 – 159 2 ND
(R)-38 I 5 0 17 – 36 0–4 12 (7.5 – 18)

(R)-3b,c H 5 0 33 – 53 0 14 (9.1 – 18)
phenytoinc 4 – 5 3 42 – 72 51 34 (21 – 45)
phenobarbitalc 20 (14 – 28)
valproatec 210 (150 – 280)
a

The compounds were tested through the auspices of the NINDS ASP.

b

Ref 23.

c

NINDS ASP internal control data.