Synthesis and preliminary biological evaluation of indol-3-yl-oxoacetamides as potent cannabinoid receptor type 2 ligands

Rareş Petru Moldovan, Winnie Deuther-Conrad, Andrew G. Horti, Peter Brust

Research output: Contribution to journalArticlepeer-review

Abstract

A small series of indol-3-yl-oxoacetamides was synthesized starting from the literature known N-(adamantan-1-yl)-2-(5-(furan-2-yl)-1-pentyl-1H-indol-3-yl)-2-oxoacetamide (5) by substituting the 1-pentyl-1H-indole subunit. Our preliminary biological evaluation showed that the fluorinated derivative 8 is a potent and selective CB2 ligand with Ki = 6.2 nM.

Original languageEnglish (US)
Article number77
JournalMolecules
Volume22
Issue number1
DOIs
StatePublished - Jan 2017

Keywords

  • Binding affinity
  • Cannabinoid receptor type 2
  • Indole
  • Positron emission tomography

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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