MAGNETIC RESONANCE IMAGING CONTRAST AGENT CAPABLE OF DETECTING HYDROGEN PEROXIDE AND REDUCING REACTIVE OXYGEN SPECIES

摘要

The current invention provides metal ion complexes with an organic ligand, compositions comprising such complexes. In particular, these complexes are capable of reacting with a reactive oxygen species in a subject and increase their T1-weighted relaxivities so a clinical MRI scanner can detect an oxidative stress hotspot in the subject. The disclosed complexes also exhibit excellent anti-oxidant properties and low cell toxicity, therefore can be used as a therapeutic agent to relieve oxidative stress in the subject, or as both a MRI contrast agent and therapeutic agent in a composition.

主权项

1. A composition comprising a complex of a metal ion M with a ligand A, or salt thereof, wherein the complex has a generic formula,
[M(A)(B)]x wherein M is Mn2+, Ni2+, Co2+, Fe2+, or a combination thereof;
B is absent, acetonitrile, methanol, Cl−, Br−, I−, ethanol, water, perchlorate, triflate, a small inorganic or organic molecule or ion, mondentate, bidentate, or a combination thereof, A is a ligand of formula IIand
x is an integer between 6 and -6, Wherein R11, R12, R13, and R14 are independently a substituted or unsubstituted pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, 1,2,3-triazinyl, 1,2,4-trazinyl, 1,3,5-triazinyl, quinolyl, phenolyl group, or an isomer thereof, and at least one of R11, R12, R13, and R14 is a substituted or unsubstituted quinolyl group.