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With a half-life of 68 min, Ga-68 is an attractive radio-metal for incorporation into PET imaging agents, since ⁶⁸Ga is produced from a commercially available ⁶⁸Ge/⁶⁸Ga generator system. Recently, our group has developed the linear chelating agent, H₂dedpa (N₄O₂) that binds Ga(III) quickly under mild conditions, and possesses ideal properties to be incorporated into a ⁶⁸Ga PET imaging agent. Herein, we report nitroimidazole(NI)-containing derivatives of H₂dedpa to investigate specific targeting of hypoxic tumour cells.

Two families of bifunctional chelators (BFCs) based on the H₂dedpa scaffold were synthesized: N-alkylated derivatives were prepared via alkylation of the 2° nitrogens of the ethylenediamine backbone with the appropriate NI targeting moiety to produce a small library of compounds, and a bifunctional derivative of H₂dedpa was prepared (H₂dedpa-Bn-NCS) to synthesize …