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EnglishOn 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.
Triazine compounds as antagonists at Bv8-prokineticin receptors / BALBONI G; LAZZARI I; TRAPELLA C; NEGRI L; LATTANZI R; GIANNINI E; NICOTRA A; MELCHIORRI P; VISENTIN S; DE NUCCIO C; SALVADORI S. - 51(2008), pp. 7635-7639.
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| Titolo: | Triazine compounds as antagonists at Bv8-prokineticin receptors |
| Autori: | |
| Data di pubblicazione: | 2008 |
| Rivista: | |
| Citazione: | Triazine compounds as antagonists at Bv8-prokineticin receptors / BALBONI G; LAZZARI I; TRAPELLA C; NEGRI L; LATTANZI R; GIANNINI E; NICOTRA A; MELCHIORRI P; VISENTIN S; DE NUCCIO C; SALVADORI S. - 51(2008), pp. 7635-7639. |
| 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. |
| Handle: | http://hdl.handle.net/11584/15498 |
| Tipologia: | 1.1 Articolo in rivista |
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