Affordable Access

deepdyve-link
Publisher Website

Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents.

Authors
  • Horton, William1
  • Sood, Abha1
  • Peerannawar, Swarada1
  • Kugyela, Nandor1
  • Kulkarni, Aditya1
  • Tulsan, Rekha1
  • Tran, Chris D1
  • Soule, Jessica1
  • LeVine, Harry 3rd2
  • Török, Béla1
  • Török, Marianna3
  • 1 University of Massachusetts Boston, 100 Morrissey Blvd., Boston, MA, USA.
  • 2 Department of Molecular and Cellular Biochemistry, Chandler School of Medicine, and Center on Aging, University of Kentucky, Lexington, KY 40536, USA.
  • 3 University of Massachusetts Boston, 100 Morrissey Blvd., Boston, MA, USA. Electronic address: [email protected]
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Jan 15, 2017
Volume
27
Issue
2
Pages
232–236
Identifiers
DOI: 10.1016/j.bmcl.2016.11.067
PMID: 27923619
Source
Medline
Keywords
License
Unknown

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.

Report this publication

Statistics

Seen <100 times