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Isaac E Marx,
Erin F DiMauro,
Alan Cheng,
Renee Emkey,
Stephen A Hitchcock,
Liyue Huang, Ming Y Huang,
Jason Human,
Josie H Lee,
Xingwen Li,
Matthew W Martin,
Ryan D White,
Robert T Fremeau,
Vinod F Patel
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ABSTRACT: A series of alpha-amidosulfones were found to be potent and selective agonists of CB(2). The discovery, synthesis, and structure-activity relationships of this series of agonists are reported. In addition, the pharmacokinetic properties of the most promising compounds are profiled.
Bioorganic & medicinal chemistry letters 12/2008; 19(1):31-5. · 2.65 Impact Factor
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Erin F DiMauro,
John L Buchanan,
Alan Cheng,
Renee Emkey,
Stephen A Hitchcock,
Liyue Huang, Ming Y Huang,
Brett Janosky,
Josie H Lee,
Xingwen Li,
Matthew W Martin,
Susan A Tomlinson,
Ryan D White,
Xiao Mei Zheng,
Vinod F Patel,
Robert T Fremeau
[show abstract]
[hide abstract]
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.
Bioorganic & medicinal chemistry letters 08/2008; 18(15):4267-74. · 2.65 Impact Factor
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Isaac E. Marx,
Erin F. DiMauro,
Alan Cheng,
Renee Emkey,
Stephen A. Hitchcock,
Liyue Huang, Ming Y. Huang,
Jason Human,
Josie H. Lee,
Xingwen Li,
Matthew W. Martin,
Ryan D. White,
Robert T. Fremeau Jr,
Vinod F. Patel
Bioorganic & Medicinal Chemistry Letters. 19(1):31-35.
