Novel methylene-linked heterocyclic EP1 receptor antagonists

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1592-7. doi: 10.1016/j.bmcl.2008.01.071. Epub 2008 Jan 19.

Abstract

We describe the SAR, in terms of heterocyclic replacements, for a series of pyrazole EP(1) receptor antagonists. This study led to the identification of several aromatic heterocyclic replacements for the pyrazole in the original compound. Investigation of replacements for the methylene linker uncovered disparate SAR in the thiazole and pyridine series.

MeSH terms

  • Heterocyclic Compounds / chemistry*
  • Heterocyclic Compounds / pharmacology*
  • Models, Molecular
  • Molecular Structure
  • Protein Binding
  • Receptors, Prostaglandin E / antagonists & inhibitors*
  • Receptors, Prostaglandin E, EP1 Subtype
  • Structure-Activity Relationship

Substances

  • Heterocyclic Compounds
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP1 Subtype