Is macrocycle a synonym for kinetic inertness in Gd(III) Complexes? Effect of coordinating and noncoordinating substituents on inertness and relaxivity of Gd(III) chelates with DO3A-like ligands.

ABSTRACT: Gadolinium chelates with octadentate ligands are widely used as contrast agents for magnetic resonance imaging (MRI), with macrocyclic ligands based on DO3A being preferred for the high kinetic inertness of their Gd chelates. A major challenge in the design of new bifunctional MRI probes is the need to control the rotational motion of the chelate, which greatly affects its relaxivity. In this work we explored facile alkylation of a secondary amine in macrocyclic DO3A-like ligands to create a short, achiral linkage to limit the undesired internal motion of chelates within larger molecular constructs. The acetate moiety on the trans nitrogen was also replaced with either a bidentate (ethoxyacetate, L1 or methyl picolinate, L2) or bulky monodentate (methyl phosphonate, L3) donor arm to give o

SUBMITTER: Polasek M 

PROVIDER: S-EPMC3640422 | biostudies-literature | 2013 Apr

REPOSITORIES: biostudies-literature