Design, synthesis and structure–activity relationship of rhenium 2-arylbenzothiazoles as β-amyloid plaque binding agents

…, NS Mason, ML Debnath, CA Mathis, WE Klunk…

文献索引：Pan, Jinhe; Mason, Neale S.; Debnath, Manik L.; Mathis, Chester A.; Klunk, William E.; Lin, Kuo-Shyan Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1720 - 1726

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被引用次数: 13

摘要

To continue our efforts toward the development of 99mTc PiB analogs, we have synthesized 24 neutral and lipophilic Re (as a surrogate of 99mTc) 2-arylbenzothiazoles, and explored their structure–activity relationship for binding to Aβ1–40 fibrils. These Re complexes were designed and synthesized via the integrated approach, so their 99mTc analogs would have a greater chance of crossing the blood–brain barrier. While the lipophilicities (logPC18= ...