title: Triazine compounds as antagonists at Bv8-prokineticin receptors.
abstract: On the basis of a Janssen's patent, we approached a new synthesis of some 1,3,5-triazin-4,6-diones as potential non peptidic prokineticin receptor antagonists, containing the following substitutions: (N(1) and N(5) link a 4-methoxybenzyl and a 4-ethylbenzyl, respectively; C(2) can link an amino-ethyl-guanidine (reference compound 1) or an ethylendiamine (2) or an amino-ethyl-amino-2-imidazoline (3). New compounds were assessed for PKR1 and PKR2 affinity. Antagonist properties were evaluated as inhibition of 1 nM Bv8-induced intracellular Ca2+ mobilization.
authors.affiliation: Department of Pharmaceutical Sciences, University of Ferrara, I-44100 Ferrara, Italy. gbalboni@unica.it
authors.forename: Gianfranco
authors.initials: G
authors.lastname: Balboni
authors.forename: Ilaria
authors.initials: I
authors.lastname: Lazzari
authors.forename: Claudio
authors.initials: C
authors.lastname: Trapella
authors.forename: Lucia
authors.initials: L
authors.lastname: Negri
authors.forename: Roberta
authors.initials: R
authors.lastname: Lattanzi
authors.forename: Elisa
authors.initials: E
authors.lastname: Giannini
authors.forename: Annalisa
authors.initials: A
authors.lastname: Nicotra
authors.forename: Pietro
authors.initials: P
authors.lastname: Melchiorri
authors.forename: Sergio
authors.initials: S
authors.lastname: Visentin
authors.forename: Chiara De
authors.initials: CD
authors.lastname: Nuccio
authors.forename: Severo
authors.initials: S
authors.lastname: Salvadori
mesh_terms: D001665:Binding Sites / Q000187:drug effects; D002118:Calcium / Q000378:metabolism; D020013:Calcium Signaling / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005768:Gastrointestinal Hormones / Q000737:chemistry; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D009479:Neuropeptides / Q000737:chemistry; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors*; D018000:Receptors, Peptide / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D005768:Gastrointestinal Hormones; D008024:Ligands; D009479:Neuropeptides; C423608:PROK2 protein, human; C470837:PROKR1 protein, human; C470838:PROKR2 protein, human; D043562:Receptors, G-Protein-Coupled; D018000:Receptors, Peptide; D014227:Triazines; D002118:Calcium