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Synthesis and affinity evaluation for AT1 receptor of phenylsalicylaldoxime-derivatives structurally related to sartans.

  作者 Rapposelli, Simona;Cuboni, Serena;Digiacomo, Maria;Lucacchini, Antonio;Minutolo, Filippo;Trincavelli, Maria Letizia;Balsamo, Aldo;  
  选自 期刊  Heterocycles;  卷期  2008年75-6;  页码  1467-1477  
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[摘要]The synthesis of new potential AT1 antagonists through the replacement of the biphenyltetrazole portion of the losartan with biphenylaldoximic and phenylsalicylaldoximic moieties was reported. Moreover, also the trifluoromethylpyrazole analog was prepd. The new compds. synthesized were evaluated for their AT1 affinity through binding assay carried out on rat liver membranes using [125I]Sar1,Ile8-angiotensina II as radioligand.

 
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