The synthesis and structure–activity relationship of substituted N-phenyl anthranilic acid analogs as amyloid aggregation inhibitors

It is believed that β-amyloid aggregation is an important event in the development of Alzheimer’s disease. In the course of our studies to identify β-amyloid aggregation inhibitors, a series of N-phenyl anthranilic acid analogs were synthesized and studied for β-amyloid inhibition activity. The synt...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-02, Vol.19 (3), p.654-657
Main Authors: Simons, Lloyd J., Caprathe, Bradley W., Callahan, Michael, Graham, James M., Kimura, Takenori, Lai, Yingjie, LeVine, Harry, Lipinski, William, Sakkab, Annette T., Tasaki, Yoshikazu, Walker, Lary C., Yasunaga, Tomoyuki, Ye, Yuyang, Zhuang, Nian, Augelli-Szafran, Corinne E.
Format: Article
Language:English
Subjects:
Alzheimer Disease
Alzheimer’s disease
Amyloid - chemistry
Amyloid aggregation
Amyloid aggregation inhibitors
Amyloid plaques
Analogs
Animals
Beta-amyloid
Biological and medical sciences
Chemistry, Pharmaceutical - methods
Disease Models, Animal
Drug Design
Enzyme Inhibitors - pharmacology
Fenamates - chemical synthesis
Fenamates - chemistry
Hsiao mouse model
Humans
Medical sciences
Mice
Microscopy, Atomic Force
Models, Chemical
Molecular Structure
N-Phenyl anthranilic acid
Neuropharmacology
Peptides - chemistry
Pharmacology. Drug treatments
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Structure-Activity Relationship
Tg2576 mice
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Summary:It is believed that β-amyloid aggregation is an important event in the development of Alzheimer’s disease. In the course of our studies to identify β-amyloid aggregation inhibitors, a series of N-phenyl anthranilic acid analogs were synthesized and studied for β-amyloid inhibition activity. The synthesis, structure–activity relationship, and in vivo activity of these analogs are discussed. It is believed that β-amyloid aggregation is an important event in the development of Alzheimer’s disease. In the course of our studies to identify β-amyloid aggregation inhibitors, a series of N-phenyl anthranilic acid analogs were synthesized and studied for β-amyloid inhibition activity. The synthesis, structure–activity relationship, and in vivo activity of these analogs are discussed.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2008.12.049