Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4450-7. doi: 10.1016/j.bmcl.2006.06.045. Epub 2006 Jun 30.

Abstract

The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited potent binding affinity and functional activity at MCH-R1, and good oral bioavailability in rat.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Molecular Structure
  • Pyrrolidines / chemical synthesis*
  • Pyrrolidines / chemistry
  • Pyrrolidines / pharmacology*
  • Rats
  • Receptors, Pituitary Hormone / antagonists & inhibitors*
  • Receptors, Pituitary Hormone / metabolism
  • Structure-Activity Relationship
  • Urea / analogs & derivatives*
  • Urea / chemical synthesis
  • Urea / chemistry
  • Urea / pharmacology

Substances

  • Pyrrolidines
  • Receptors, Pituitary Hormone
  • melanin-concentrating hormone receptor
  • Urea