Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands

Himanshu Bhattacharjee, Steven N. Gurley, Bob Moore

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

A novel series of cannabinoid ligands with a structurally unique tri-aryl core has been designed, synthesized and assayed. Receptor binding assays show that these compounds possess CB2 receptor sub-type selectivity with binding affinities ranging from 1.07 (±0.05) for 7 to 4.77 (±0.57) nM for 6. The selectivity of the compounds was enhanced 9-600-fold for the CB2 receptor over the CB1 receptor. The results of our present study identify a novel, highly selective cannabinoid scaffold with a non-classical core.

Original languageEnglish (US)
Pages (from-to)1691-1693
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number6
DOIs
StatePublished - Mar 15 2009

Fingerprint

Cannabinoid Receptor CB2
Cannabinoids
Ligands
Cannabinoid Receptor CB1
Scaffolds
Assays

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Clinical Biochemistry
  • Molecular Biology
  • Molecular Medicine
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands. / Bhattacharjee, Himanshu; Gurley, Steven N.; Moore, Bob.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 6, 15.03.2009, p. 1691-1693.

Research output: Contribution to journalArticle

Bhattacharjee, Himanshu ; Gurley, Steven N. ; Moore, Bob. / Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 6. pp. 1691-1693.
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