Synthesis and structure–activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists

…, MS Domalski, WJ Greenlee, K O'Neill…

Index: Wu, Wen-Lian; Burnett, Duane A.; Spring, Richard; Qiang, Li; Sasikumar, Thavalakulamgara K.; Domalski, Martin S.; Greenlee, William J.; O'Neill, Kim; Hawes, Brian E. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 14 p. 3668 - 3673

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Citation Number: 7

Abstract

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.