Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB(2)

Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.42). 08/2008; 18(15):4267-74. DOI: 10.1016/j.bmcl.2008.06.096
Source: PubMed


Structural modifications to the central portion of the N-arylamide oxadiazole scaffold led to the identification of N-arylpiperidine oxadiazoles as conformationally constrained analogs that offered improved stability and comparable potency and selectivity. The simple, modular scaffold allowed for the use of expeditious and divergent synthetic routes, which provided two-directional SAR in parallel. Several potent and selective agonists from this novel ligand class are described. (c) 2008 Elsevier Ltd. All rights reserved.

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