Triazine compounds as antagonists at Bv8-prokineticin receptors

BALBONI, GIANFRANCO;LAZZARI I;TRAPELLA C;NEGRI L;LATTANZI R;GIANNINI E;NICOTRA A;MELCHIORRI P;VISENTIN S;DE NUCCIO C;SALVADORI S.

2008-01-01

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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.