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

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3668-73. doi: 10.1016/j.bmcl.2006.04.061. Epub 2006 May 11.

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.

MeSH terms

  • Humans
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacology*
  • Receptors, Pituitary Hormone / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Piperidines
  • Receptors, Pituitary Hormone
  • melanin-concentrating hormone receptor