Bioorganic & Medicinal Chemistry Letters 2005-08-15

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

Tao Guo, Yuefei Shao, Gang Qian, Laura L Rokosz, Tara M Stauffer, Rachael C Hunter, Suresh D Babu, Huizhong Gu, Doug W Hobbs

Index: Bioorg. Med. Chem. Lett. 15 , 3696, (2005)

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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.