Identification and hit-to-lead optimization of a novel class of CB1 antagonists
Letourneau, Jeffrey J and Jokiel, Patrick and Olson, John and Riviello, Christopher M and Ho, Koc-Kan and McAleer, Lihong and Yang, Jingchun and Swanson, Robert N and Baker, James and Cowley, Phillip and Edwards, Darren and Ward, Nick and Ohlmeyer, Michael H J and Webb, Maria L (2010) Identification and hit-to-lead optimization of a novel class of CB1 antagonists. Bioorganic and Medicinal Chemistry Letters, 20 (18). pp. 5449-5453. ISSN 0960-894X (https://doi.org/10.1016/j.bmcl.2010.07.091)
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The discovery, synthesis and preliminary structure-activity relationships (SARs) of a novel class of CB1 antagonists is described. Initial optimization of benzimidazole-based screening hit 4 led to the identification of 'inverted' indole-based lead compound 18c with improved properties versus compound 4 including reduced AlogP, improved microsomal stability and improved aqueous solubility. Compound 18c demonstrates in vivo CB1 antagonist efficacy (CB1 agonist induced hypothermia model) and is orally bioavailable in rat.
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Item type: Article ID code: 49475 Dates: DateEvent15 September 2010PublishedSubjects: Medicine > Other systems of medicine
Technology > Chemical technology
Medicine > Pharmacy and materia medicaDepartment: Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences Depositing user: Pure Administrator Date deposited: 01 Oct 2014 15:15 Last modified: 08 Apr 2024 21:41 Related URLs: URI: https://strathprints.strath.ac.uk/id/eprint/49475