Oxorhenium(V) and Oxotechnetium(V) Complexes of N3S Tetradentate Ligands with a Styrylpyridyl Functional Group: Toward Imaging Agents to Assist in the Diagnosis of Alzheimer's Disease

Inorg Chem. 2021 Sep 6;60(17):13669-13680. doi: 10.1021/acs.inorgchem.1c01992. Epub 2021 Aug 23.

Abstract

Alzheimer's disease (AD) is associated with the presence of amyloid plaques in the brain mainly comprised of aggregated forms of amyloid-β (Aβ). Molecules radiolabeled with technetium-99m that cross the blood-brain barrier (BBB) and selectively bind to Aβ plaques have the potential to assist in the diagnosis of AD using single-photon emission computed tomography imaging. In this work, three new tetradentate ligands of pyridyl, amide, amine and thiol donors, featuring a styrylpyridyl group that is known to interact with amyloid plaques, were prepared. The new ligands formed charge-neutral and lipophilic complexes with the [Tc═O]3+ and [Re═O]3+ motifs, and two rhenium complexes were characterized by X-ray crystallography. The rhenium(V) complexes interact with synthetic Aβ1-40 and amyloid plaques on human brain tissue. Two of the new ligands were radiolabeled with 99mTc using a kit-based approach, and their biodistribution in wild-type mice was evaluated. The presence of amide donors in the tetradentate ligand increased the stability of the respective [Tc═O]3+ complexes but reduced brain uptake. While the complexes were able to cross the BBB, the degree of uptake in the brain was not sufficient to justify further investigation of these complexes.

MeSH terms

  • Alzheimer Disease / diagnostic imaging*
  • Alzheimer Disease / metabolism
  • Amyloid beta-Peptides / metabolism
  • Animals
  • Brain / diagnostic imaging
  • Coordination Complexes / chemical synthesis
  • Coordination Complexes / chemistry*
  • Coordination Complexes / metabolism
  • Coordination Complexes / pharmacokinetics
  • Humans
  • Ligands
  • Mice
  • Organotechnetium Compounds / chemical synthesis
  • Organotechnetium Compounds / chemistry*
  • Organotechnetium Compounds / metabolism
  • Organotechnetium Compounds / pharmacokinetics
  • Peptide Fragments / metabolism
  • Pyridines / chemical synthesis
  • Pyridines / chemistry
  • Pyridines / metabolism
  • Pyridines / pharmacokinetics
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / metabolism
  • Radiopharmaceuticals / pharmacokinetics
  • Rhenium / chemistry
  • Styrenes / chemical synthesis
  • Styrenes / chemistry
  • Styrenes / metabolism
  • Styrenes / pharmacokinetics

Substances

  • Amyloid beta-Peptides
  • Coordination Complexes
  • Ligands
  • Organotechnetium Compounds
  • Peptide Fragments
  • Pyridines
  • Radiopharmaceuticals
  • Styrenes
  • amyloid beta-protein (1-40)
  • Rhenium