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Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.

Authors :
Mezeiova E
Hrabinova M
Hepnarova V
Jun D
Janockova J
Muckova L
Prchal L
Kristofikova Z
Kucera T
Gorecki L
Chalupova K
Kunes J
Hroudova J
Soukup O
Korabecny J
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Jul 01; Vol. 43, pp. 128100. Date of Electronic Publication: 2021 May 10.
Publication Year :
2021

Abstract

The search for novel and effective therapeutics for Alzheimer's disease (AD) is the main quest that remains to be resolved. The goal is to find a disease-modifying agent able to confront the multifactorial nature of the disease positively. Herewith, a family of huprineY-tryptophan heterodimers was prepared, resulting in inhibition of cholinesterase and neuronal nitric oxide synthase enzymes, with effect against amyloid-beta (Aβ) and potential ability to cross the blood-brain barrier. Their cholinesterase pattern of behavior was inspected using kinetic analysis in tandem with docking studies. These heterodimers exhibited a promising pharmacological profile with strong implication in AD.<br /> (Copyright © 2021 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
43
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
33984470
Full Text :
https://doi.org/10.1016/j.bmcl.2021.128100