2. Academic Validation
  3. Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties

Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties

  • J Med Chem. 2003 May 22;46(11):2110-6. doi: 10.1021/jm020329q.
Stephen T Wrobleski 1,  Ping Chen,  John Hynes Jr,  Shuqun Lin,  Derek J Norris,  Chennagiri R Pandit,  Steven Spergel,  Hong Wu,  John S Tokarski,  Xiaorong Chen,  Kathleen M Gillooly,  Peter A Kiener,  Kim W McIntyre,  Vina Patil-Koota,  David J Shuster,  Lori A Turk,  Guchen Yang,  Katerina Leftheris
Affiliations

Affiliation

  • 1 Department of Discovery Chemistry, Bristol-Myers Squibb, P.O. Box 4000, Princeton, New Jersey 08543-4000, USA. stephen.wrobleski@bms.com
PMID: 12747783 DOI: 10.1021/jm020329q
Abstract

A series of unique indazoles and pyridoindolones have been rationally designed and synthesized as novel classes of cannabinoid ligands based on a proposed bioactive amide conformation. This has led to the discovery of the novel indolopyridone 3a as a conformationally constrained cannabinoid ligand that displays high affinity for the CB2 receptor (K(i)(CB2) = 1.0 nM) and possesses antiinflammatory properties when administered orally in an in vivo murine inflammation model.

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