Abstract
The synthesis of a new series of imidazo[2,1-b]thiazole derivatives is described. They were tested as potential acetylcholinesterase and butyrylcholinesterase inhibitors by means of a chemiluminescent microassay. Although most of the new compounds did not show significant cholinesterase inhibition potency, three of them displayed selective antiacetylcholinesterase activity in the micromolar range.
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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Acylation
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Alkylation
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Animals
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Benzene / chemistry
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Binding Sites
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Butyrylcholinesterase / metabolism*
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Cholinesterase Inhibitors / chemical synthesis*
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Cholinesterase Inhibitors / chemistry
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Cholinesterase Inhibitors / metabolism
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Cholinesterase Inhibitors / pharmacology*
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Dose-Response Relationship, Drug
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Drug Design
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / metabolism
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Imidazoles / pharmacology*
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Inhibitory Concentration 50
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Kinetics
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Luminescent Measurements*
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
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Thiazoles / metabolism
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Thiazoles / pharmacology*
Substances
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Cholinesterase Inhibitors
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Imidazoles
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Thiazoles
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Acetylcholinesterase
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Butyrylcholinesterase
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Benzene