Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity

  • Bioorg Med Chem Lett. 2008 Mar 1;18(5):1725-9. doi: 10.1016/j.bmcl.2008.01.042.
Monika Ermann  1 ,  Doris Riether ,  Edward R Walker ,  Innocent F Mushi ,  James E Jenkins ,  Beatriz Noya-Marino ,  Mark L Brewer ,  Malcolm G Taylor ,  Patricia Amouzegh ,  Stephen P East ,  Brian W Dymock ,  Mark J Gemkow ,  Andreas F Kahrs ,  Andreas Ebneth ,  Sabine Löbbe ,  Kathy O'Shea ,  Daw-Tsun Shih ,  David Thomson
Affiliations
  • 1. Evotec (UK) Ltd., 114 Milton Park, Abingdon, Oxfordshire OX14 4SA, United Kingdom. [email protected]
PMID: 18255291 DOI: 10.1016/j.bmcl.2008.01.042
Abstract

A high-throughput screening campaign resulted in the discovery of a highly potent dual Cannabinoid Receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified.