Abstract
On the basis of N-((5-(3-(1-benzylpiperidin-4-yl)propoxy)-1-methyl-1H-indol-2-yl)methyl)-N-methylprop-2-yn-1-amine (II, ASS234) and QSAR predictions, in this work we have designed, synthesized, and evaluated a number of new indole derivatives from which we have identified N-methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine (2, MBA236) as a new cholinesterase and monoamine oxidase dual inhibitor.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Blood-Brain Barrier / drug effects
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Brain / drug effects
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Brain / enzymology
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Cell Membrane Permeability / drug effects
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Cholinesterase Inhibitors / chemical synthesis
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Cholinesterase Inhibitors / pharmacology*
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Cholinesterases / chemistry*
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Indoles / chemical synthesis
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Indoles / pharmacology*
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Models, Molecular
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Molecular Structure
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Monoamine Oxidase / chemistry*
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Monoamine Oxidase Inhibitors / chemical synthesis
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Monoamine Oxidase Inhibitors / pharmacology*
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Piperidines / chemical synthesis
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Piperidines / pharmacology*
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Swine
Substances
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Cholinesterase Inhibitors
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Indoles
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Monoamine Oxidase Inhibitors
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N-methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine
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Piperidines
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Monoamine Oxidase
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Cholinesterases