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Bioorganic & medicinal chemistry

Dibenzothiazoles as novel amyloid-imaging agents

C Wu, J Wei, K Gao, Y Wang

文献索引:Wu, Chunying; Wei, Jingjun; Gao, Kuanqiang; Wang, Yanming Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 7 p. 2789 - 2796

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被引用次数: 36

摘要

Novel dibenzothiazole derivatives were synthesized and evaluated as amyloid-imaging agents. In vitro quantitative binding studies using AD brain tissue homogenates showed that the dibenzothiazole derivatives displayed high binding affinities with Ki values in the nanomolar range (6.8–36nM). These derivatives are relatively lipophilic with partition coefficients (logP oct) in the range of 1.25–3.05. Preliminary structure–activity relationship ...