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Triazine Compounds as Antagonists at Bv8-Prokineticin Receptors.

  作者 Balboni, Gianfranco;Lazzari, Ilaria;Trapella, Claudio;Negri, Lucia;Lattanzi, Roberta;Giannini, Elisa;Nicotra, Annalisa;Melchiorri, Pietro;Visentin, Sergio;De Nuccio, Chiara;Salvadori, Severo;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-23;  页码  7635-7639  
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[摘要]We approached a new synthesis of some 1,3,5-triazine-4,6-diones as potential non peptidic prokineticin receptor antagonists, contg. the following substitutions: N1 and N5 are linked to 4-methoxybenzyl and 4-ethylbenzyl groups; C2 is linked to an amino-ethyl-guanidine or an amino-ethyl-amino-2-imidazoline group. New compds. were assessed for PKR1 and PKR2 affinity. Antagonist properties were evaluated as inhibition of 1 nM Bv8-induced intracellular Ca2+ mobilization.

 
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