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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Binding Sites / drug effects
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Calcium / metabolism
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Calcium Signaling / drug effects
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Dose-Response Relationship, Drug
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Drug Design
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Gastrointestinal Hormones / chemistry
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Humans
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Ligands
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Molecular Structure
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Neuropeptides / chemistry
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Receptors, G-Protein-Coupled / antagonists & inhibitors*
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Receptors, Peptide / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
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Triazines / chemical synthesis
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Triazines / chemistry
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Triazines / pharmacology*
Substances
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Gastrointestinal Hormones
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Ligands
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Neuropeptides
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PROK2 protein, human
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PROKR1 protein, human
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PROKR2 protein, human
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Receptors, G-Protein-Coupled
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Receptors, Peptide
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Triazines
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Calcium