117471-01-9Relevant academic research and scientific papers
The anticonvulsant activities of functionalized N-benzyl 2-acetamidoacetamides. The importance of the 2-acetamido substituent
Choi, Daeock,Stables, James P.,Kohn, Harold
, p. 2105 - 2114 (1996)
Recent studies have demonstrated that substituted N-benzyl 2-acetamidoacetamides provide significant protection against maximal electroshock (MES)-induced seizures in mice and rats. In this study, we investigated whether the 2-acetamido moiety was necessary for anticonvulsant activity. Ten derivatives of the known anticonvulsant, N-benzyl 2-acetamido-2-phenylacetamide were prepared in which the 2-acetamido group was replaced by hydrogen, methyl, oxygen, and halogen substituents. Evaluation of these compounds in the MES-induced seizure test demonstrated that both the hydroxy and the methoxy compounds provided full protection against MES-induced seizures in mice given ip at 100 mg/g. Moreover, evaluation of the individual stereoisomers for the hydroxy compound showed that the principal activity resided in the (R)-isomer. These findings demonstrated that the 2-acetamido substituent is important but not obligatory for the prevention of MES-induced seizures. Further supporting evidence was provided by comparing the pharmacological activities of N-benzyl 2,3-dimethoxypropionamide with N-benzyl 2-acetamido-3-methoxypropionamide. The ED50 value for the former in the MES test was 3.0 mg/kg (ip), which compared favorably with phenobarbital (ED50=22 mg/kg), but the ED50 value for N-benzyl 2-acetamido-3-methoxypropionamide was 8.3 mg/kg.
Metal-ligand cooperation in the catalytic dehydrogenative coupling (DHC) of polyalcohols to carboxylic acid derivatives
Trincado, Monica,Kuehlein, Klaus,Gruetzmacher, Hansjoerg
supporting information; experimental part, p. 11905 - 11913 (2011/11/06)
Several polyols, which are easily available from sugars through biochemical conversion or hydrogenolytic cleavage, are directly converted into carboxylic acids and amides. This efficient dehydrogenative coupling process, catalyzed by a rhodium(I) diolefin amido complex, is an attractive approach for the production of organic fine chemicals from renewable resources. This method tolerates the presence of several hydroxy groups and can be extended to the direct synthesis of lactams from the corresponding amino alcohols under mild conditions.
Propionamide anticonvulsants
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, (2008/06/13)
The present invention is directed to a compound of the following formula: STR1 pharmaceutical compositions containing the same and the use thereof as an anticonvulsant.
