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Novel benzimidazole derivatives as selective CB2 agonists
Authors:Pagé Daniel  Balaux Elise  Boisvert Luc  Liu Ziping  Milburn Claire  Tremblay Maxime  Wei Zhongyong  Woo Simon  Luo Xuehong  Cheng Yun-Xing  Yang Hua  Srivastava Sanjay  Zhou Fei  Brown William  Tomaszewski Miroslaw  Walpole Christopher  Hodzic Leila  St-Onge Stéphane  Godbout Claude  Salois Dominic  Payza Kemal  Payza Keymal
Affiliation:Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada. daniel.page@astrazeneca.com
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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