Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids.
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.
Connolly
P J
PJ
The R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869, USA. pconnoll@prius.jnj.com
Wetter
S K
SK
Murray
W V
WV
Johnson
D L
DL
McMahon
F J
FJ
Farrell
F X
FX
Tullai
J
J
Jolliffe
L K
LK
D000596:Amino Acids / Q000138:chemical synthesis* / Q000378:metabolism; D019281:Dimerization; D017467:Receptors, Erythropoietin / Q000378:metabolism*
D000596:Amino Acids; D017467:Receptors, Erythropoietin