Ono, Masahiro Watanabe, Rumi Kawashima, Hidekazu Cheng, Yan Kimura, Hiroyuki Watanabe, Hiroyuki Haratake, Mamoru Saji, Hideo Nakayama, Morio Fluoro-pegylated Chalcones as Positron Emission Tomography Probes for in Vivo Imaging of β-Amyloid Plaques in Alzheimer’s Disease This paper describes the synthesis and biological evaluation of fluoro-pegylated (FPEG) chalcones for the imaging of β-amyloid (Aβ) plaques in patients with Alzheimer’s disease (AD). FPEG chalcone derivatives were prepared by the aldol condensation reaction. In binding experiments conducted in vitro using Aβ(1−42) aggregates, the FPEG chalcone derivatives having a dimethylamino group showed higher <i>K</i><sub>i</sub> values (20−50 nM) than those having a monomethylamino or a primary amine group. When the biodistribution of <sup>11</sup>C-labeled FPEG chalcone derivatives having a dimethyamino group was examined in normal mice, all four derivatives were found to display sufficient uptake for imaging Aβ plaques in the brain. <sup>18</sup>F-labeled <b>7c</b> also showed good uptake by and clearance from the brain, although a slight difference between the <sup>11</sup>C and <sup>18</sup>F tracers was observed. When the labeling of Aβ plaques was carried out using brain sections of AD model mice and an AD patient, the FPEG chalcone derivative <b>7c</b> intensely labeled Aβ plaques. Taken together, the results suggest <b>7c</b> to be a useful candidate PET tracer for detecting Aβ plaques in the brain of patients with AD. FPEG chalcone derivatives;Positron Emission Tomography Probes;uptake;β plaques;AD model mice;aldol condensation reaction;Alzheimer;imaging;7 c;candidate PET tracer;18 F tracers 2009-10-22
    https://acs.figshare.com/articles/journal_contribution/Fluoro_pegylated_Chalcones_as_Positron_Emission_Tomography_Probes_for_in_Vivo_Imaging_of_Amyloid_Plaques_in_Alzheimer_s_Disease/2819206
10.1021/jm901057p.s001