Benzylphenylpyrrolizinones with Anti-amyloid and Radical Scavenging Effects, Potentially Useful in Alzheimer's Disease Treatment

ChemMedChem. 2017 Jun 21;12(12):913-916. doi: 10.1002/cmdc.201700102. Epub 2017 Apr 12.

Abstract

Herein we describe the drug design steps developed to increase the radical scavenging and β-amyloid aggregation inhibitory activities of a previously described series of benzylidenephenylpyrrolizinones. Among the newly synthesized derivatives, some benzylphenylpyrrolizinones exhibited interesting results in regard to those activities. Initial druggability parameters were measured, and suggest these compounds as a suitable starting point for potential alternatives in treating Alzheimer's disease.

Keywords: Alzheimer′s disease; MTDL; antioxidants; pyrrolizinones; β-amyloid.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-2 Receptor Antagonists / chemical synthesis
  • Adrenergic alpha-2 Receptor Antagonists / chemistry
  • Adrenergic alpha-2 Receptor Antagonists / pharmacology*
  • Alzheimer Disease / drug therapy*
  • Amyloid beta-Peptides / antagonists & inhibitors*
  • Dose-Response Relationship, Drug
  • Drug Design
  • Free Radical Scavengers / chemical synthesis
  • Free Radical Scavengers / chemistry
  • Free Radical Scavengers / pharmacology*
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Protein Aggregates / drug effects
  • Pyrrolizidine Alkaloids / chemical synthesis
  • Pyrrolizidine Alkaloids / chemistry
  • Pyrrolizidine Alkaloids / pharmacology*
  • Structure-Activity Relationship

Substances

  • Adrenergic alpha-2 Receptor Antagonists
  • Amyloid beta-Peptides
  • Free Radical Scavengers
  • Protein Aggregates
  • Pyrrolizidine Alkaloids