Thiosemicarbazonate complexes with affinity for amyloid-ß fibers: synthesis, characterization and biological studies.
Future Med Chem
; 11(19): 2527-2546, 2019 10.
Article
in En
| MEDLINE
| ID: mdl-31633404
ABSTRACT
Aim:
Obtain radioimages of amyloid-ß fibers using 99mTc-complexes.Methodology:
Tridentate thiosemicarbazone and thiocarbonohydrazone ligands containing fragments (stilbene, azobenzene, benzothiazole or benzoxazole) with affinity for amyloid-ß fibers and its Re(I) complexes have been prepared. The molecular structures of several ligands and complexes were determined by x-ray diffraction. Binding affinity studies toward Aß1-42 fibers were performed for the ligands and Re(I) complexes. The ability of formation of some 99mTc(I) complexes, their biodistribution and in vivo stability have been established. Results &conclusion:
Complexes of stilbene and benzothiazole thiosemicarbazonates show similar affinity for amyloid-ß fibers to the free ligand. These 99mTc complexes present a reasonable in vivo stability and a low capability to cross the blood-brain barrier although not sufficient to brain amyloid imaging.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Thiosemicarbazones
/
Brain
/
Amyloid beta-Peptides
/
Radiopharmaceuticals
Limits:
Humans
Language:
En
Journal:
Future Med Chem
Year:
2019
Document type:
Article