| Literature DB >> 27923619 |
William Horton1, Abha Sood1, Swarada Peerannawar1, Nandor Kugyela1, Aditya Kulkarni1, Rekha Tulsan1, Chris D Tran1, Jessica Soule1, Harry LeVine2, Béla Török1, Marianna Török3.
Abstract
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.Entities:
Keywords: Alzheimer’s disease; Amyloid beta; Antioxidant; Cholinesterase inhibition; β-Carbolines
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Year: 2016 PMID： 27923619 PMCID： PMC5282889 DOI： 10.1016/j.bmcl.2016.11.067
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823