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Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids
P J Connolly1, S K Wetter, W V Murray
1The R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869, USA. pconnoll@prius.jnj.com
Bioorganic & Medicinal Chemistry Letters
|September 15, 2000
Abstract:
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 microM) affinity for EBP; 'dimerization' of the most potent analogues by coupling with linear diamines led to EPO competitors having 1-2 microM binding affinities.