Author/Authors :
Erin F. DiMauro، نويسنده , , John L. Buchanan، نويسنده , , Alan Cheng، نويسنده , , Renee Emkey، نويسنده , , Stephen A. Hitchcock، نويسنده , , Liyue Huang، نويسنده , , Ming Y. Huang، نويسنده , , Brett Janosky، نويسنده , , Josie H. Lee، نويسنده , , Xingwen Li، نويسنده , , Matthew W. Martin، نويسنده , , Susan A. Tomlinson، نويسنده , , Ryan D. White، نويسنده , , Xiao Mei Zheng، نويسنده , , Vinod F. Patel، نويسنده , , Robert T. Fremeau Jr.، نويسنده ,
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.
