Synthesis of a Novel Library of 2H-Indazole Analogues as Potential Binders of B-Amyloid Plaques


Alzheimer’s disease is a progressive brain disorder that is characterized by gradual loss of memory and the ability to learn and comprehend. The aggregates of β-amyloid are considered one of the most prominent pathological hallmarks of the disease. Thus, efforts towards the diagnosis of the disease focused on the development of biomarkers that selectively bind to β-amyloid aggregates. The most successful biomarker that caught much attention and is undergoing extensive clinical trials is Pittsburgh compound [11C]PiB, a Positron Emission Tomography (PET) imaging agent. In this work, we report the synthetic optimization and characterization of a small library of 2H-indazoles bearing structural similarities to [11C]PiB. These analogues will be accessed through the Davis-Beirut reaction where a suitable linker will be synthesized and incorporated onto the C3 position of the indazole ring.


El Dakdouki M.H.


Huang X., Hussein A.R.

Journal/Conference Information

21th LAAS International Scientific Conference,