[(18)F]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of beta-amyloid fibrils.
In this study a novel series of isoindol-1-one and isoindol-1,3-dione derivatives for beta-amyloid-specific binding agents is described. Twelve compounds were synthesized and evaluated via a competitive binding assay with [(125)I]TZDM against beta-amyloid 1-42 (Abeta42) aggregates. Two new [(18)F]-labeled isoindole derivatives were synthesized and evaluated as potential beta-amyloid imaging probes based on the in vivo pharmacokinetic profiles. The preliminary results suggest that these [(18)F]18b and [(18)F]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of Abeta fibrils in the brains of Alzheimer's disease (AD) patients.
Center for Chemoinformatics Research, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, South Korea.
Ji Hoon
JH
Lee
Seong Rim
SR
Byeon
YoungSoo
Y
Kim
Soo Jeong
SJ
Lim
Seung Jun
SJ
Oh
Dae Hyuk
DH
Moon
Kyung Ho
KH
Yoo
Bong Young
BY
Chung
Dong Jin
DJ
Kim
D000682:Amyloid / Q000737:chemistry*; D016229:Amyloid beta-Peptides / Q000737:chemistry*; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000187:drug effects; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D005462:Fluorine Radioisotopes / Q000494:pharmacology*; D006801:Humans; D054833:Isoindoles / Q000737:chemistry*; D007700:Kinetics; D051379:Mice; D008956:Models, Chemical; D058225:Plaque, Amyloid / Q000187:drug effects; D049268:Positron-Emission Tomography / Q000295:instrumentation* / Q000379:methods
D000682:Amyloid; D016229:Amyloid beta-Peptides; D005462:Fluorine Radioisotopes; D054833:Isoindoles