Synthesis of MRI contrast agents derived from DOTAM-Gly- l-Phe-OH incorporating a disulfide bridge: Conjugation to a cell penetrating peptide and preparation of a dimeric agent

Abstract

A cell penetrating peptide conjugate and dimeric PARACEST MRI contrast agents, based on the DOTAM-Gly- l-Phe-OH scaffold have been prepared in moderate yields using diethyl azodicarboxylate (DEAD) or iodine-mediated disulfide bridge formation as a key step. Magnetic (PARACEST) properties of these agents have been evaluated.