N-Substituted amino acid N′-benzylamides: Synthesis, anticonvulsant, and metabolic activities

C Béguin, A LeTiran, JP Stables, RD Voyksner…

Index: Beguin, Cecile; LeTiran, Arnaud; Stables, James P.; Voyksner, Robert D.; Kohn, Harold Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 11 p. 3079 - 3096

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Citation Number: 24

Abstract

Amino acid amides (AAA) were prepared and evaluated in seizure models. The AAA displayed moderate-to-excellent activity in the maximal electroshock seizure (MES) test and were devoid of activity in the subcutaneous Metrazol-induced (scMet) seizure test. The AAA anticonvulsant activity was neither strongly influenced by the C (2) substituent nor by the degree of terminal amine substitution. An in vitro metabolism study suggested that the ...