Available online 24 December 2013
In Press, Corrected Proof — Note to users
Benzimidazole CB2 agonists: Design, synthesis and SAR
- Kausik K. Nandaa,
, 
, - Darrell A. Henzeb,
- Kimberly Della Pennab,
- Reshma Desaib,
- Michael Leitlb,
- Wei Lemaireb,
- Rebecca B. Whitec,
- Suzie Yehc,
- Janine N. Brouilletted,
- George D. Hartmana,
- Mark T. Bilodeaua,
- B. Wesley Trottere
- a Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA, United States
- b Department of Pain Research, Merck Research Laboratories, West Point, PA, United States
- c Department of Drug Metabolism & Pharmacokinetics, Merck Research Laboratories, West Point, PA, United States
- d Department of Structure Elucidation, Merck Research Laboratories, West Point, PA, United States
- e Department of Medicinal Chemistry, Merck Research Laboratories, Boston, MA, United StatesAbstract
A new series of CB2-selective agonists containing a benzimidazole core is reported. Design, synthesis, SAR and pharmacokinetic data for selected compounds are described.
Graphical abstract
Keywords
- CB2 agonist;
- Cannabinoid 2 receptor;
- Benzimidazole
Figures and tables from this article:
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Figure 1.
Imidazopyridine CB2 agonists.
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Figure 2.
Design of benzimidazole core from imidazopyridine scaffold.
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Figure 3.
Overlay of gas phase conformations (within 3 kcal/mol of global minimum) of imidazopyridine 3 and benzimidazole 12.
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Figure 4.
PK (dog cassette) data. amL/min/kg; bh; cL/kg.
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Scheme 1.
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Scheme 2.
- Corresponding author. Tel.: +1 2156520371.
Copyright © 2013 Elsevier Ltd. All rights reserved.
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When the final article is assigned to an issue of the journal, the Article in Press version will be removed and the final version will appear in the associated published issue of the journal. The date the article was first made available online will be carried over.
