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J Med Chem. 2008 Dec 11;51(23):7635-9. doi: 10.1021/jm800854e.

Triazine compounds as antagonists at Bv8-prokineticin receptors.

Author information

  • 1Department of Pharmaceutical Sciences, University of Ferrara, I-44100 Ferrara, Italy. gbalboni@unica.it

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.

PMID:
19006379
[PubMed - indexed for MEDLINE]
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