New derivatives of benzylamide with anticonvulsant activity.

نویسندگان

  • Marzanna Strupińska
  • Grazyna Rostafińska-Suchar
  • James P Stables
  • Ryszard Paruszewski
چکیده

Previously obtained picolinic acid benzylamide is a potent anticonvulsant with low neurotoxicity. In search for new effective anticonvulsants twelve new benzylamides (1-12) were synthesized and preliminary evaluated in the Anticonvulsant Screening Program (ASP) of Antiepileptic Drug Development Program (ADDP) of NIH. Two of them appeared the most promising: 1-cyclopentenecarboxylic acid benzylamide (1-Cpc-BZA) (9) showed MES ED50 = 85,36 mg/kg (PI = 2,49), scPTZ ED50 = 1,37 mg/kg (PI = 1,37), 6Hz-EST ED50 = 50,29 mg/kg and cyclopentanecarboxylic acid benzylamide (Cpc-BZA) (11) showed pilocarpine ED50 = 154.75 mg/kg and pilocarpine ED97 = 270.95 mg/kg.

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عنوان ژورنال:
  • Acta poloniae pharmaceutica

دوره 66 2  شماره 

صفحات  -

تاریخ انتشار 2009