Triazinediones as prokineticin 1 receptor antagonists. Part 1: SAR, synthesis and biological evaluation

Janet L Ralbovsky; Joseph G Lisko; Jeffrey M Palmer; John Mabus; Kristen M Chevalier; Mark J Schulz; Alexey B Dyatkin; Tamara A Miskowski; Steven J Coats; Pamela Hornby; Wei He

doi:10.1016/j.bmcl.2009.03.157

Triazinediones as prokineticin 1 receptor antagonists. Part 1: SAR, synthesis and biological evaluation

Bioorg Med Chem Lett. 2009 May 15;19(10):2661-3. doi: 10.1016/j.bmcl.2009.03.157. Epub 2009 Apr 5.

Authors

Janet L Ralbovsky¹, Joseph G Lisko, Jeffrey M Palmer, John Mabus, Kristen M Chevalier, Mark J Schulz, Alexey B Dyatkin, Tamara A Miskowski, Steven J Coats, Pamela Hornby, Wei He

Affiliation

¹ Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L. L. C., Spring House, PA 19477, United States. jralb@msn.com

PMID: 19375913
DOI: 10.1016/j.bmcl.2009.03.157

Abstract

A series of guanidine triazinediones were identified as potent PK1 receptor antagonists. A compound in this series inhibited the PK1 invoked prosecretory response in rat ileum tissue.

MeSH terms

Animals
Cell Line
Humans
Rats
Receptors, G-Protein-Coupled / antagonists & inhibitors*
Receptors, G-Protein-Coupled / metabolism
Structure-Activity Relationship
Triazines / chemical synthesis*
Triazines / chemistry
Triazines / pharmacology

Substances

PROKR1 protein, human
Receptors, G-Protein-Coupled
Triazines