2. Academic Validation
  3. Novel benzimidazole derivatives as selective CB2 agonists

Novel benzimidazole derivatives as selective CB2 agonists

  • Bioorg Med Chem Lett. 2008 Jul 1;18(13):3695-700. doi: 10.1016/j.bmcl.2008.05.073.
Daniel Pagé 1,  Elise Balaux,  Luc Boisvert,  Ziping Liu,  Claire Milburn,  Maxime Tremblay,  Zhongyong Wei,  Simon Woo,  Xuehong Luo,  Yun-Xing Cheng,  Hua Yang,  Sanjay Srivastava,  Fei Zhou,  William Brown,  Miroslaw Tomaszewski,  Christopher Walpole,  Leila Hodzic,  Stéphane St-Onge,  Claude Godbout,  Dominic Salois,  Kemal Payza
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada. daniel.page@astrazeneca.com
PMID: 18522867 DOI: 10.1016/j.bmcl.2008.05.073
Abstract

The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to excellent selectivity (>1000-fold) over the CB1 receptor.

Figures
Products