Abstract
Acetylcholinesterase (AChE) inhibitors played an important role in developing a cure for Alzheimer' s disease. In order to study on the influence of modifications at different groups and side chains on the AChE inhibitory ability and the active sites of 7H-thiazolo[3,2-b][1,2,4]triazin-7-one derivatives, fourteen 3,6-diaryl-7H-thiazolo[3,2-b][1,2,4]triazin-7-one derivatives were designed and synthesized. The study of AChE inhibitory activity was carried out using the Ellman colorimetric assay with huperzine-A as the positive control drug. Most of the target compounds exhibited more than 50% inhibition at 10 μM. Some target compounds showed strong inhibition against AChE. The molecular fields analysis and preliminary structure-activity relationships are discussed.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylcholinesterase / chemistry*
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Acetylcholinesterase / metabolism*
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Alzheimer Disease / drug therapy
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Animals
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Binding Sites
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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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Databases, Protein
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GPI-Linked Proteins / antagonists & inhibitors
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GPI-Linked Proteins / chemistry
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GPI-Linked Proteins / metabolism
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Humans
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Magnetic Resonance Spectroscopy
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Models, Molecular
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Molecular Conformation
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Protein Binding
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Spectrometry, Mass, Electrospray Ionization
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Spectrophotometry, Infrared
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Structure-Activity Relationship
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Thiazoles / chemistry
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Torpedo / metabolism
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Triazines / chemistry
Substances
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Cholinesterase Inhibitors
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GPI-Linked Proteins
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Thiazoles
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Triazines
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ACHE protein, human
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Acetylcholinesterase