Title

Novel benzimidazole derivatives as selective CB2 agonists

Authors

Luc Boisvert, University of Puget SoundFollow
Daniel Pagé, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Elise Balaux, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Ziping Liu, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Claire Milburn, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Maxime Tremblay, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Zhongyong Wei, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Simon Woo, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Xuehong Luo, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Yun-Xing Cheng, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Hua Yang, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Sanjay Srivastava, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Fei Zhou, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
William Brown, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Miroslaw Tomaszewski, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Christopher Walpole, Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Leila Hodzic, Department of Molecular Pharmacology, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Stéphane St-Onge, Department of Molecular Pharmacology, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Claude Godbout, Department of Molecular Pharmacology, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Dominic Salois, Department of Molecular Pharmacology, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9
Keymal Payza, Department of Molecular Pharmacology, AstraZeneca R&D Montréal, 7171 Frederick-Banting, St-Laurent, Que., Canada H4S 1Z9

Document Type

Article

Publication Date

2008

Publication Title

Bioorganic & Medicinal Chemistry Letters

Department

Chemistry

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 1 nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to excellent selectivity (>1000-fold) over the CB1 receptor.

ISSN

0960-894X