The design and synthesis of novel NK1/NK2 dual antagonists

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2329-32. doi: 10.1016/s0960-894x(00)00463-7.

Abstract

Functional probing of the backbone of the Sanofi NK2 antagonist SR 48968 has resulted in the discovery of two new classes of NK1/NK2 dual antagonists: the diamine class and the oxime class. The addition of the amino or the oxime functional group results in the reversal of the stereochemical preference of the NK2 receptor.

MeSH terms

  • Animals
  • Benzamides / chemical synthesis*
  • Benzamides / chemistry*
  • Benzamides / pharmacology
  • Diamines / chemical synthesis*
  • Diamines / chemistry
  • Diamines / pharmacology
  • Drug Design
  • Kinetics
  • Molecular Structure
  • Neurokinin-1 Receptor Antagonists*
  • Oximes / chemical synthesis*
  • Oximes / chemistry
  • Oximes / pharmacology
  • Piperidines / chemical synthesis*
  • Piperidines / chemistry*
  • Piperidines / pharmacology
  • Receptors, Neurokinin-2 / antagonists & inhibitors*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Benzamides
  • Diamines
  • Neurokinin-1 Receptor Antagonists
  • Oximes
  • Piperidines
  • Receptors, Neurokinin-2
  • SR 48968