Moerlein S M, Welch M J, Raymond K N, Weitl F L
J Nucl Med. 1981 Aug;22(8):710-9.
Isopropyl N-substituted tricatecholamide analogs of enterobactin have been found to form gallium and indium complexes with very high stability constants and to exhibit in vivo characteristics significantly different from gallium- or indium-transferrin and EDTA. The 3,4-DiP-LICAMS and TiP-MECAMS complexes were found to clear primarily through the kidneys, whereas the less polar 3,4-DiP-LICAM complex was eliminated through the liver. The rationale for developing new metal-binding analogs with larger organic groups attached to the amide nitrogens is discussed.
已发现肠杆菌素的异丙基N-取代三儿茶酚酰胺类似物能形成具有非常高稳定常数的镓和铟配合物，并且在体内表现出与镓-或铟-转铁蛋白以及EDTA显著不同的特性。发现3,4-二异丙基-赖氨酸酰胺（3,4-DiP-LICAMS）和三异丙基-甲氧基儿茶酚酰胺（TiP-MECAMS）配合物主要通过肾脏清除，而极性较小的3,4-二异丙基-赖氨酸酰胺（3,4-DiP-LICAM）配合物则通过肝脏消除。文中讨论了开发在酰胺氮上连接有较大有机基团的新型金属结合类似物的基本原理。
