Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1)

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2171-8. doi: 10.1016/j.bmcl.2007.01.104. Epub 2007 Feb 4.

Abstract

The design, synthesis, and SAR of a series of substituted spirohydantoins are described. Optimization of an in-house screening hit gave compounds that exhibited potent binding affinity and functional activity at MCH-R1.

Publication types

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

MeSH terms

  • Anti-Obesity Agents / chemical synthesis*
  • Anti-Obesity Agents / pharmacology
  • Drug Design
  • Humans
  • Hydantoins / chemical synthesis*
  • Hydantoins / pharmacology
  • Kinetics
  • Protein Binding
  • Receptors, Pituitary Hormone / antagonists & inhibitors*
  • Spiro Compounds / chemical synthesis*
  • Spiro Compounds / pharmacology
  • Structure-Activity Relationship

Substances

  • Anti-Obesity Agents
  • Hydantoins
  • Receptors, Pituitary Hormone
  • Spiro Compounds
  • melanin-concentrating hormone receptor