Triazinediones as prokineticin 1 receptor antagonists. Part 1: SAR, synthesis and biological evaluation.
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.
Ralbovsky
Janet L
JL
Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L. L. C., Spring House, PA 19477, United States. jralb@msn.com
Lisko
Joseph G
JG
Palmer
Jeffrey M
JM
Mabus
John
J
Chevalier
Kristen M
KM
Schulz
Mark J
MJ
Dyatkin
Alexey B
AB
Miskowski
Tamara A
TA
Coats
Steven J
SJ
Hornby
Pamela
P
He
Wei
W
D000818:Animals; D002460:Cell Line; D006801:Humans; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
C470837:PROKR1 protein, human; D043562:Receptors, G-Protein-Coupled; D014227:Triazines