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 Ca(2+) mobilization.
Triazine Compounds as Antagonists at Bv8-Prokineticin Receptors / Gianfranco, Balboni; Ilaria, Lazzari; Claudio, Trapella; Negri, Lucia; Lattanzi, Roberta; Giannini, Elisa; Nicotra, Annalisa; Melchiorri, Pietro; Sergio, Visentin; C., De Nuccio; Severo, Salvadori. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 51:23(2008), pp. 7635-7639. [10.1021/jm800854e]
Triazine Compounds as Antagonists at Bv8-Prokineticin Receptors
NEGRI, Lucia;LATTANZI, Roberta;GIANNINI, Elisa;NICOTRA, ANNALISA;MELCHIORRI, Pietro;
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: (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 Ca(2+) mobilization.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
