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
  • 1. Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada. [email protected]
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.

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