Abstract
Background: Alzheimer's disease is a chronic neurodegenerative chronic disease with a heavy social and economic impact in our developed societies, which still lacks an efficient therapy. Method: This paper describes the Hantzsch multicomponent synthesis of twelve alkyl hexahydro-quinoline-3-carboxylates, 4a-l, along with the evaluation of their Ca2+ channel blockade capacity, cholinesterase inhibition and antioxidant power. Results: Compound 4l showed submicromolar inhibition of butyrylcholinesterase, Ca2+ channel antagonism and an antioxidant effect. Conclusion: Compound 4l is an interesting compound that deserves further investigation for Alzheimer's disease therapy.
Keywords:
Alzheimer's disease; Hantzsch multicomponent reaction; antioxidants; calcium channel blockers; cholinesterase inhibitors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylcholinesterase / metabolism
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Animals
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Antioxidants / chemical synthesis
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Antioxidants / chemistry
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Antioxidants / pharmacology*
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Benzaldehydes / chemical synthesis
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Benzaldehydes / chemistry
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Benzaldehydes / pharmacology*
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Butyrylcholinesterase / metabolism
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Calcium Channel Blockers / chemical synthesis
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Calcium Channel Blockers / chemistry
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Calcium Channel Blockers / pharmacology*
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Calcium Channels / metabolism*
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Cholinesterase Inhibitors / chemical synthesis
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Cholinesterase Inhibitors / chemistry
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Cholinesterase Inhibitors / pharmacology*
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Electrophorus
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Horses
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Humans
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Quinolines / chemical synthesis
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Quinolines / chemistry
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Quinolines / pharmacology*
Substances
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Antioxidants
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Benzaldehydes
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Calcium Channel Blockers
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Calcium Channels
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Cholinesterase Inhibitors
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Quinolines
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Acetylcholinesterase
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Butyrylcholinesterase
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benzaldehyde