Abstract
The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Abeta fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Abeta fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC(50)=0.07 and 0.08 microM, respectively) than those of Curcumin (IC(50)=0.80 microM) and IMSB (IC(50)=8.00 microM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alzheimer Disease / drug therapy
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Alzheimer Disease / metabolism
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Amyloid beta-Peptides / antagonists & inhibitors
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Amyloid beta-Peptides / chemistry*
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Benzofurans / chemical synthesis*
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Benzofurans / pharmacology
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Benzothiazoles
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Benzoxazoles / chemistry
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Chemistry, Pharmaceutical / methods*
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Curcumin / chemical synthesis
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Curcumin / pharmacology
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Drug Design
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Electrons
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Humans
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Inhibitory Concentration 50
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Models, Chemical
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Peptide Fragments / antagonists & inhibitors*
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Peptide Fragments / chemistry
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Structure-Activity Relationship
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Styrenes / chemical synthesis*
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Styrenes / pharmacology
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Thiazoles / chemistry
Substances
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1-iodo-2,5-bis-(3-hydroxycarbonyl-4-methoxy)styryl-benzene
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Amyloid beta-Peptides
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Benzofurans
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Benzothiazoles
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Benzoxazoles
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Peptide Fragments
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Styrenes
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Thiazoles
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amyloid beta-protein (1-42)
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thioflavin T
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Curcumin
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benzofuran