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

Bioorg Med Chem Lett. 2009 Feb 1;19(3):654-7. doi: 10.1016/j.bmcl.2008.12.049. Epub 2008 Dec 24.

Abstract

It is believed that beta-amyloid aggregation is an important event in the development of Alzheimer's disease. In the course of our studies to identify beta-amyloid aggregation inhibitors, a series of N-phenyl anthranilic acid analogs were synthesized and studied for beta-amyloid inhibition activity. The synthesis, structure-activity relationship, and in vivo activity of these analogs are discussed.

MeSH terms

  • Alzheimer Disease
  • Amyloid / chemistry*
  • Animals
  • Chemistry, Pharmaceutical / methods*
  • Disease Models, Animal
  • Drug Design
  • Enzyme Inhibitors / pharmacology
  • Fenamates / chemical synthesis
  • Fenamates / chemistry*
  • Humans
  • Mice
  • Microscopy, Atomic Force
  • Models, Chemical
  • Molecular Structure
  • Peptides / chemistry
  • Structure-Activity Relationship

Substances

  • Amyloid
  • Enzyme Inhibitors
  • Fenamates
  • Peptides