Benzimidazole CB2 agonists: design, synthesis and SAR

Kausik K Nanda; Darrell A Henze; Kimberly Della Penna; Reshma Desai; Michael Leitl; Wei Lemaire; Rebecca B White; Suzie Yeh; Janine N Brouillette; George D Hartman; Mark T Bilodeau; B Wesley Trotter

doi:10.1016/j.bmcl.2013.12.068

Benzimidazole CB2 agonists: design, synthesis and SAR

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1218-21. doi: 10.1016/j.bmcl.2013.12.068. Epub 2013 Dec 25.

Authors

Affiliations

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA, United States. Electronic address: [email protected].
² Department of Pain Research, Merck Research Laboratories, West Point, PA, United States.
³ Department of Drug Metabolism & Pharmacokinetics, Merck Research Laboratories, West Point, PA, United States.
⁴ Department of Structure Elucidation, Merck Research Laboratories, West Point, PA, United States.
⁵ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA, United States.
⁶ Department of Medicinal Chemistry, Merck Research Laboratories, Boston, MA, United States.

PMID: 24461289
DOI: 10.1016/j.bmcl.2013.12.068

Abstract

A new series of CB2-selective agonists containing a benzimidazole core is reported. Design, synthesis, SAR and pharmacokinetic data for selected compounds are described.

Keywords: Benzimidazole; CB2 agonist; Cannabinoid 2 receptor.

MeSH terms

Benzimidazoles / chemical synthesis
Benzimidazoles / chemistry
Benzimidazoles / pharmacology*
Dose-Response Relationship, Drug
Drug Design*
Humans
Models, Molecular
Molecular Structure
Receptor, Cannabinoid, CB2 / agonists*
Structure-Activity Relationship

Substances

Benzimidazoles
Receptor, Cannabinoid, CB2
benzimidazole