Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids

被引：7

作者：

Connolly, PJ ^{[1
]}

Wetter, SK ^{[1
]}

Murray, WV ^{[1
]}

Johnson, DL ^{[1
]}

McMahon, FJ ^{[1
]}

Farrell, FX ^{[1
]}

Tullai, J ^{[1
]}

Jolliffe, LK ^{[1
]}

机构：

[1] RW Johnson Pharmaceut Res Inst, Raritan, NJ 08869 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(00)00399-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N, N-Dicinnamyl, N-benzyl-N-cinnamyl, and N, N-dibenzyl amino acids were prepared and evaluated in an EPO binding assay. Several derivatives of aspartic acid, glutamic acid, and lysine exhibited moderate (10 50 mu M) affinity for EBP; 'dimerization' of the most potent analogues by coupling with linear diamines led to EPO competitors having 1-2 mu M binding. affinities. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1995 / 1999

页数：5

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