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Preparation and anticonvulsant activity of a series of functionalized. alpha.-aromatic and. alpha.-heteroaromatic amino acids

…, P LeGall, JD Conley, DW Robertson…

文献索引:Kohn, Harold; Sawhney, Kailash N.; LeGall, Philippe; Conley, Judith D.; Robertson, David W.; Leander, J. David Journal of Medicinal Chemistry, 1990 , vol. 33, # 3 p. 919 - 926

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被引用次数: 58

摘要

We recently reported the potent anticonvulsant activity of (R, S)-a-acetamido-N-benzyl-a- phenylacetamide(2b). Selectively substituted derivatives of this compound have now been prepared (23 examples) and evaluated in the maximal electroshock seizure (MES) and horizontal screen (tox) tests in mice. In several key cases, replacement of the a-phenyl substituent in 2b by a relatively small, electron-rich, heteroaromatic moiety led to a ...