"Novel benzimidazole derivatives as selective CB2 agonists" by Luc Boisvert, Daniel Pagé et al.

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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

DOI

http://dx.doi.org/10.1016/j.bmcl.2008.05.073

WorldCat Link

http://worldcat.org/oclc/264468105

Provider Link

http://www.sciencedirect.com/science/article/pii/S0960894X08005817

Citation

Page?, D, E Balaux, L Boisvert, Z Liu, C Milburn, M Tremblay, Z Wei, S Woo, X Luo, YX Cheng, H Yang, S Srivastava, F Zhou, W Brown, M Tomaszewski, C Walpole, L Hodzic, S St-Onge, C Godbout, D Salois, and K Payza. "Novel Benzimidazole Derivatives As Selective Cb2 Agonists." Bioorganic & Medicinal Chemistry Letters. 18.13 (2008): 3695-700. Print.

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