108267-41-0Relevant academic research and scientific papers
Intermediates for anticonvulsant agents
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, (2008/06/13)
This invention provides certain 4-acylamino benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.
Synthesis and Anticonvulsant Activity of Analogues of 4-Amino-N-(1-phenylethyl)benzamide
Clark, C. Randall,Davenport, Timothy W.
, p. 1214 - 1218 (2007/10/02)
A group of amides and amines related to 4-amino-N-(1-phenylethyl)benzamide, 1, were prepared in a study on the relationship of structure to anticonvulsant activity in this compound. Acylation and alkylation of the amino group of 1 resulted in almost total loss of anticonvulsant activity. Insertion of a methylene between the 4-amino group and the aromatic ring of 1 produced a slight increase in anticonvulsant potency and a significant increase in toxicity. Hydride reduction of the amide carbonyl in 1 also yielded compounds having a slightly lower ED50 against convulsions induced by electroshock and a much lower TD50 in the rotorod assay. Modification of the 1-phenylethyl group of 1 also decreased anticonvulsant potency.
