Novel chalcones as probes for in vivo imaging of β-amyloid plaques in Alzheimer’s brains
摘要:
A novel series of chalcone derivatives for in vivo imaging beta-amyloid plaques in the brain of Alzheimer's disease (AD) were synthesized and characterized. When in vitro binding studies using A beta aggregates were carried out with chalcone derivatives, the binding affinities for A aggregate varied from 3 to 105 nM. The radioiodinated chalcones were successfully prepared through an iododestannylation reaction from the corresponding tributyltin derivatives using hydrogen peroxide as the oxidant in high yields and with high radiochemical purities. Biodistribution studies in normal mice after iv injection of the radioiodinated chalcones displayed high brain uptake (2.0-4.7%ID/g at 2 min) and rapid clearance from the brain (0.2-0.6%ID/g at 30 min), which is highly desirable or amyloid imaging agents. The results in this study suggest that the novel radioiodinated chalcones may be useful amyloid imaging agents for detecting P-amyloid plaques in the brain of AD. (C) 2007 Elsevier Ltd. All rights reserved.
Totally 38 aryl E 2-propen-1-ones including nine substituted styryl 4-iodophenyl ketones have been synthesised using solvent-free SiO2-H3PO4 catalyzed Aldol condensation between respective methyl ketones and substituted benzaldehydes under microwave irradiation. The yields of the ketones are more than 80%. The synthesised chalcones were characterized by their analytical, physical and spectroscopic