1148028-92-5Relevant articles and documents
Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents
Horton, William,Sood, Abha,Peerannawar, Swarada,Kugyela, Nandor,Kulkarni, Aditya,Tulsan, Rekha,Tran, Chris D.,Soule, Jessica,LeVine, Harry,T?r?k, Béla,T?r?k, Marianna
, p. 232 - 236 (2016/12/27)
The design, synthesis and assessment of β-carboline core-based compounds as potential multifunctional agents against several processes that are believed to play a significant role in Alzheimer's disease (AD) pathology, are described. The activity of the compounds was determined in Aβ self-assembly (fibril and oligomer formation) and cholinesterase (AChE, BuChE) activity inhibition, and their antioxidant properties were also assessed. To obtain insight into the mode of action of the compounds, HR-MS studies were carried out on the inhibitor-Aβ complex formation and molecular docking was performed on inhibitor-BuChE interactions. While several compounds exhibited strong activities in individual assays, compound 14 emerged as a promising multi-target lead for the further structure-activity relationship studies.