N-substituted amino acid N′-benzylamides:: synthesis, anticonvulsant, and metabolic activities

被引：23

作者：

Béguin, C

LeTiran, A

Stables, JP

Voyksner, RD

Kohn, H

机构：

[1] Univ N Carolina, Div Med Chem & Nat Prod, Sch Pharm, Chapel Hill, NC 27599 USA

[2] Univ Houston, Dept Chem, Houston, TX 77204 USA

[3] NINDS, Epilepsy Branch, NIH, Rockville, MD 20852 USA

[4] LCMS Ltd, Raleigh, NC 27611 USA

[5] Univ N Carolina, Sch Pharm, Div Med Chem & Nat Prod, Chapel Hill, NC 27599 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 11期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1016/j.bmc.2004.02.043

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 structure-activity relationship pattern was due, in part, to metabolic processes that occurred at the N-terminal amine unit. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：3079 / 3096

页数：18

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