Sulfonamide linker-based inhibitors with extended linear structure were designed and synthesized with the aim of producing multifunctional agents against several processes involved in the pathology of Alzheimer's disease (AD). The potency of the compounds were assessed in the inhibition of Aβ self-assembly (fibril and oligomer formation), in modulating cholinesterase (AChE, BuChE) activity, and scavenging free radicals. Several compounds exhibited promising Aβ self-assembly and cholinesterase inhibition and in parallel, showed good free radical scavenging properties. The investigation of the scaffold described in this study resulted in the identification of three compounds (14, 19 and 26) as promising leads for the further design of multifunctional drug candidates for AD.
|Number of pages||5|
|Journal||Bioorganic and Medicinal Chemistry Letters|
|State||Published - Feb 1 2015|
Bibliographical noteFunding Information:
Financial support provided by the University of Massachusetts Boston through the 2013 Joseph P. Healey Research Grant and National Institute of Health ( R21AG028816-01 to H.L.) is gratefully acknowledged.
© 2014 Elsevier Ltd. All rights reserved.
- Alzheimer's disease
- Amyloid-β Cholinesterase inhibition
ASJC Scopus subject areas
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry