Аннотация:In this work we presented a synthesis and investigation ofrelative acyclic and macrocyclic polyamines with picolinate pendantarms as potential chelators for copper radiopharmaceuticals. It hasbeen shown that linear chelators lacking bisamide moiety are muchmore basic and form complexes with higher stability constantscompared to macrocyclic ones. Both types of ligands possess manydonor sites due to picolinate groups enabling formation of polynuclearcomplexes in the solution and solid state. According to crystalstructures metal cations coordinates with studied ligands through thebinding with aminogroups and picolinates donor atoms, while terminalaminogroups of acyclic ligands do not take part in the complexformation. Tripicolinate azacrown ligand coordinates cations outsidethe macrocyclic cavity in non-equivalent positions. However this outcagelocation as well as a moderate logK value do not induce fastrelease of cation from this complex in the challenging medium ofserum proteins.
