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Note | Regular issue | Vol 75, No. 6, 2008, pp.1467-1477
Published online, 12th February, 2008
DOI: 10.3987/COM-07-11309
Synthesis and Affinity Evaluation for AT1 Receptor of Phenylsalicylaldoxime-Derivatives Structurally Related to Sartans

Simona Rapposelli,* Serena Cuboni, Maria Digiacomo, Antonio Lucacchini, Filippo Minutolo, Maria Letizia Trincavelli, and Aldo Balsamo

*Department of Medicinal Chemistry, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy

Abstract

In this work we reported the synthesis of new potential AT1 antagonists through the replacement of the biphenyltetrazole portion of the losartan with biphenylaldoximic (2) and phenylsalicylaldoximic (3a) moieties. Moreover, also the trifluoromethylpyrazole analogue of 3a (3b) was prepared. The new compounds synthesized were evaluated for their AT1 affinity through binding assay carried out on rat liver membranes using [125I]Sar1,Ile8-angiotensina II as radioligand.