N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4432-6. doi: 10.1016/j.bmcl.2007.06.022. Epub 2007 Jun 10.

Abstract

A series of N-alkylbenzenesulfonamides were developed from a high throughput screening hit. Classic and parallel synthesis strategies were employed to produce compounds with good in vitro and in vivo gamma-secretase activity.

MeSH terms

  • Amyloid Precursor Protein Secretases / antagonists & inhibitors*
  • Amyloid beta-Peptides / metabolism
  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Mice
  • Mice, Transgenic
  • Molecular Structure
  • Protein Binding
  • Sulfonamides / chemistry*
  • Sulfonamides / pharmacology*

Substances

  • Amyloid beta-Peptides
  • Sulfonamides
  • Amyloid Precursor Protein Secretases