کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10588411 | 981454 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Fluorescent 2-styrylpyridazin-3(2H)-one derivatives as probes targeting amyloid-beta plaques in Alzheimer's disease
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Amyloid plaques, which are primarily composed of aggregated amyloid-beta (Aβ) peptide, are the neuropathological hallmarks of Alzheimer's disease (AD). Fluorescent markers containing 2-styrylpyridazin-3(2H)-ones were developed to detect intracellular aggregated Aβ peptides. Nine compounds exhibited a greater than 10-fold increase of in emission spectra before and after mixing with Aβ aggregates compared with before mixing. Among these compounds, compound 9n exhibited the highest affinity for Aβ aggregates (Kd = 1.84 μM) and selectively stained both aggregated intracellular Aβ and Aβ plaques in the transgenic AD model mice (APP/PS1). These preliminary results indicate that 2-styrylpyridazin-3(2H)-one derivatives are promising alternative fluorescence imaging agent for the study of AD.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 12, 15 June 2012, Pages 4106-4110
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 12, 15 June 2012, Pages 4106-4110
نویسندگان
Yong Dae Park, Jeong Hoon Park, Min Goo Hur, Sang Wook Kim, Jung-Joon Min, Seung-Hwan Park, Yung Joon Yoo, Yong-Jin Yoon, Seung Dae Yang,