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Synthesis and structure-activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists. 2006
Wen-Lian Wu, and
Duane A Burnett, and
Richard Spring, and
Li Qiang, and
Thavalakulamgara K Sasikumar, and
Martin S Domalski, and
William J Greenlee, and
Kim O'Neill, and
Brian E Hawes
Schering Plough Research Institute, 2015 Galloping Hill Road, MS 2800, Kenilworth, NJ 07033-0539, USA. wen-lian.wu@spcorp.com
Isosteric replacement of the urea group of lead compound 1 led to novel substituted piperidine phenylamide analogues. SAR on the electron-induced effects of various linkers as well as substituents on the phenyl rings and the piperidine nitrogen has been investigated. Many single-digit nanomolar MCH R1 antagonists have been identified from this series.
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