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

Lloyd J. Simons, Bradley W. Caprathe, Michael Callahan, James M. Graham, Takenori Kimura, Yingjie Lai, Harry LeVine, William Lipinski, Annette T. Sakkab, Yoshikazu Tasaki, Lary C. Walker, Tomoyuki Yasunaga, Yuyang Ye, Nian Zhuang, Corinne E. Augelli-Szafran

Research output: Contribution to journalArticlepeer-review

48 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)654-657
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number3
DOIs
StatePublished - Feb 1 2009

Keywords

  • Alzheimer's disease
  • Amyloid aggregation
  • Amyloid aggregation inhibitors
  • Amyloid plaques
  • Analogs
  • Beta-amyloid
  • Hsiao mouse model
  • N-Phenyl anthranilic acid
  • Tg2576 mice

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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