Synthesis of benzothiazole derivatives and their binding characteristics with beta-amyloid].

Lin Zhou, Chang-Sheng Gan, Hao-Shu Wang, Zhen-Zhen Zhao, Jian Pan

Engineering Research Center of Bio-process, Ministry of Education, Hefei University of Technology, Hefei 230009, China.

Yao xue xue bao = Acta pharmaceutica Sinica 2012 May

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Alzheimer's disease (AD) is a progressive neurodegenerative disease endangering human health seriously. Recent reports have revealed that beta-amyloid aggregates play a key role in the pathogenesis of AD. Thus, targeting the Abeta plaques benzothiazole derivatives were synthesized with the scaffold of the most promising imaging agent PIB ([11C]-6-OH-BTA-1, [11C]-2-(4-(methylamino)phenyl)-6-hydroxybenzothiazole) and C = N as linker to study the binding characteristics with the target protein through surface plasmon resonance (SPR) technique. These derivatives were synthesized through simple yet effective method with high yields and characterized by 1H NMR and FTIR. The binding properties (K(D)) were determined with Biacore X-100 instrument according to the fitting-plot curve. Compounds 3a and 3f showed high binding affinity for Abeta1-40. The results suggest that benzothiazole derivatives could be served as a scaffold to develop novel beta-amyloid imaging agents for the diagnosis of AD.

Citation

Lin Zhou, Chang-Sheng Gan, Hao-Shu Wang, Zhen-Zhen Zhao, Jian Pan. Synthesis of benzothiazole derivatives and their binding characteristics with beta-amyloid]. Yao xue xue bao = Acta pharmaceutica Sinica. 2012 May;47(5):685-8