Author/Authors :
Tao Guo، نويسنده , , Yuefei Shao، نويسنده , , Gang Qian، نويسنده , , Laura L. Rokosz، نويسنده , , Tara M. Stauffer، نويسنده , , Rachael C. Hunter، نويسنده , , Suresh D. Babu، نويسنده , , Huizhong Gu، نويسنده , , Doug W. Hobbs، نويسنده ,
Abstract :
An encoded combinatorial library based on aryl and biaryl piperidine scaffolds was designed and synthesized. Screening of this library resulted in the discovery of high-nanomolar biaryl piperidine-based MCH1 receptor antagonists. Follow-up optimization using a parallel synthesis provided potent, single digit nanomolar antagonists.
Keywords :
MCH , obesity , MCH1R antagonists , Encoded combinatorial synthesis