Fluorescent 2-styrylpyridazin-3(2H)-one derivatives as probes targeting amyloid-beta plaques in Alzheimer's disease

Bioorganic & Medicinal Chemistry Letters
Yong Dae ParkSeung Dae Yang

Abstract

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 (K(d)=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.

References

Nov 4, 2006·Science·Erik D Roberson, Lennart Mucke
Jul 12, 2011·ACS Chemical Neuroscience·Willy M ChangEmmanuel A Theodorakis

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Citations

Mar 22, 2016·Acta Pharmacologica Sinica·Ming-Ming XuHai-Yan Zhang
May 28, 2015·Archives of Pharmacal Research·Seung-Jin JungYong Dae Park
Apr 24, 2018·Journal of Analytical Methods in Chemistry·Yong Dae ParkSeung Sik Lee
May 26, 2018·The Journal of Organic Chemistry·Mingwei ZhouXuhong Qian

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