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•Huprine-tryptophan hybrids showed nanomolar inhibitory potency of cholinesterases.•Huprine-tryptophan hybrids inhibited the formation of Aβ1-42 aggregates.•The most potent inhibitor showed comparable anti-Aβ activity with reference myricetin.•HupY-Trp heterodimers were effective inhibitors of nNOS comparable to bis(7)-THA.
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.