N,N ',N '',N '''-tetraalkylcyclam derivatives: Synthesis, Tc-99m-labelling, and biological properties

Abstract

We synthesized N,N ' ,N " ,N ' ' ' -tetraalkylcyclam derivatives in which alkyl groups were ethyl, propyl, butyl, methoxyethyl, and ethoxyethyl. We attempted to label the compounds with Tc-99m. The cyclams with methyl, ethyl, and propyl could be labelled. The labelled N,N ' ,N " ,N ' ' ' -tetraalkylcyclam derivatives showed +1 charge. They excreted rapidly through the kidney in mice. The liver-uptake increased slightly as the lipophilicity increased. However, the myocardial uptake was low unlikely with the +1 charged myocardial imaging agents.