Article

Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.

Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 08/2008; 18(15):4267-74. DOI:10.1016/j.bmcl.2008.06.096 pp.4267-74
Source: PubMed

ABSTRACT 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.

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Keywords

comparable potency
 
conformationally constrained analogs
 
expeditious
 
N-arylamide oxadiazole scaffold
 
provided two-directional SAR
 
selective agonists
 
selectivity
 
Structural modifications