1089681-55-9Relevant academic research and scientific papers
Structure-Activity Relationship Study of Heterocyclic Phenylethenyl and Pyridinylethenyl Derivatives as Tau-Imaging Agents That Selectively Detect Neurofibrillary Tangles in Alzheimers Disease Brains
Matsumura, Kenji,Ono, Masahiro,Kitada, Ayane,Watanabe, Hiroyuki,Yoshimura, Masashi,Iikuni, Shimpei,Kimura, Hiroyuki,Okamoto, Yoko,Ihara, Masafumi,Saji, Hideo
, p. 7241 - 7257 (2015/10/05)
In order to explore novel tau-imaging agents that can selectively detect neurofibrillary tangles in Alzheimers disease (AD) brains, we designed and synthesized a series of heterocyclic phenylethenyl and (3-pyridinyl)ethenyl derivatives with or without a dimethyl amino group. In in vitro autoradiography using AD brain sections, all radioiodinated ligands with a dimethyl amino group bound to Aβ deposits in the sections. In contrast, the ligands without a dimethyl amino group showed different patterns of radioactivity accumulation in the sections depending on the kind of heterocycle contained in their molecules. Particularly, a phenylethenyl benzimidazole derivative ([125I]64) showed marked radioactivity accumulation in the temporal lobe which corresponded with the distribution of tau deposits. [125I]64 also showed the most favorable pharmacokinetics in normal mouse brains (3.69 and 0.06% ID/g at 2 and 60 min postinjection, respectively) among all ligands in this study. Taken together, these results suggest that [123I]64 may be a new candidate tau-imaging agent.
Radioactive iodine labeled compound, and, radioactive pharmaceutical containing the same (by machine translation)
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, (2018/10/10)
PROBLEM TO BE SOLVED: and compatibility and affinity for both amyloidosis acryloyldimethyltauric, labeled compd. radioactive iodine. SOLUTION: the present invention, N, N-labeled compd. dimethyl benzene amine including radioactive iodine or its salt. Selected drawing: no (by machine translation)
Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation
Byun, Ji Hun,Kim, HyeYun,Kim, YoungSoo,Mook-Jung, Inhee,Kim, Dong Jin,Lee, Won Koo,Yoo, Kyung Ho
scheme or table, p. 5591 - 5593 (2009/06/18)
The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Aβ fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Aβ fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC50 = 0.07 and 0.08 μM, respectively) than those of Curcumin (IC50 = 0.80 μM) and IMSB (IC50 = 8.00 μM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.
