Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry

Bioorg Med Chem Lett. 2001 Mar 12;11(5):747-9. doi: 10.1016/s0960-894x(01)00056-7.

Abstract

Potent and selective EP3 receptor ligands were found by making a library using solid-support chemistry. These compounds can be obtained by a Suzuki coupling reaction of a solid-supported benzyl bromide using various boronic acids. The yields obtained for this reaction were in the range of 24-95% of arylmethyl cinnamic acid 1 after cleavage from the Wang resin.

MeSH terms

  • Cinnamates / chemical synthesis*
  • Cinnamates / chemistry
  • Cinnamates / metabolism*
  • Cinnamates / pharmacology
  • Combinatorial Chemistry Techniques*
  • Humans
  • Ligands
  • Molecular Structure
  • Receptors, Prostaglandin E / antagonists & inhibitors*
  • Receptors, Prostaglandin E / chemistry
  • Receptors, Prostaglandin E / metabolism*
  • Receptors, Prostaglandin E, EP3 Subtype
  • Structure-Activity Relationship

Substances

  • Cinnamates
  • Ligands
  • PTGER3 protein, human
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP3 Subtype
  • cinnamic acid