Aminostyrylbenzofuran derivatives as potent inhibitors for Abeta fibril formation

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5591-3. doi: 10.1016/j.bmcl.2008.08.111. Epub 2008 Sep 3.

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

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / drug therapy
  • Alzheimer Disease / metabolism
  • Amyloid beta-Peptides / antagonists & inhibitors
  • Amyloid beta-Peptides / chemistry*
  • Benzofurans / chemical synthesis*
  • Benzofurans / pharmacology
  • Benzothiazoles
  • Benzoxazoles / chemistry
  • Chemistry, Pharmaceutical / methods*
  • Curcumin / chemical synthesis
  • Curcumin / pharmacology
  • Drug Design
  • Electrons
  • Humans
  • Inhibitory Concentration 50
  • Models, Chemical
  • Peptide Fragments / antagonists & inhibitors*
  • Peptide Fragments / chemistry
  • Structure-Activity Relationship
  • Styrenes / chemical synthesis*
  • Styrenes / pharmacology
  • Thiazoles / chemistry

Substances

  • 1-iodo-2,5-bis-(3-hydroxycarbonyl-4-methoxy)styryl-benzene
  • Amyloid beta-Peptides
  • Benzofurans
  • Benzothiazoles
  • Benzoxazoles
  • Peptide Fragments
  • Styrenes
  • Thiazoles
  • amyloid beta-protein (1-42)
  • thioflavin T
  • Curcumin
  • benzofuran