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ID: ALA1142772

Journal: Bioorg Med Chem Lett

Title: Discovery and SAR of biaryl piperidine MCH1 receptor antagonists through solid-phase encoded combinatorial synthesis.

Authors: Guo T, Shao Y, Qian G, Rokosz LL, Stauffer TM, Hunter RC, Babu SD, Gu H, Hobbs DW.

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.

CiteXplore: 15978811

DOI: 10.1016/j.bmcl.2005.05.085