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

• Published in: Bioorganic & medicinal chemistry letters Vol. 19; no. 10; pp. 2661 - 2663
• Main Authors: Ralbovsky, Janet L., Lisko, Joseph G., Palmer, Jeffrey M., Mabus, John, Chevalier, Kristen M., Schulz, Mark J., Dyatkin, Alexey B., Miskowski, Tamara A., Coats, Steven J., Hornby, Pamela, He, Wei
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 15.05.2009; Elsevier
• Subjects: Animals; Biological and medical sciences; Cell Line; Digestive system; Humans; Medical sciences; Neuropharmacology; Neurotransmitters. Neurotransmission. Receptors; Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems; Pharmacology. Drug treatments; PK1; Prokineticin; Rats; Receptors, G-Protein-Coupled - antagonists & inhibitors; Receptors, G-Protein-Coupled - metabolism; Structure-Activity Relationship; Triazinediones; Triazines - chemical synthesis; Triazines - chemistry; Triazines - pharmacology; Prokineticin; Triazinediones; PK1; Rat; Rodentia; Smooth muscle; Guanidines; Ileum; In vitro; Prokineticin receptor 1; Vertebrata; Mammalia; Structure activity relation; G protein coupled receptor; Animal; Antagonist; Fluorine Organic compounds; Chemical synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2009.03.157

A series of guanidine triazinediones ( 2) were identified as potent PK1 receptor antagonists. A compound in this series inhibited the PK1 invoked prosecretory response in rat ileum tissue. 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.