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: (N1 and N5 link a 4-methoxybenzyl and a 4-ethylbenzyl, respectively; C2 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.
Triazine Compounds as Antagonists at Bv8-Prokineticin Receptors
TRAPELLA, Claudio;SALVADORI, Severo
2008
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: (N1 and N5 link a 4-methoxybenzyl and a 4-ethylbenzyl, respectively; C2 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.File in questo prodotto:
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