In this work we reported thy 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]Sarl,Ile8-angiotensina II as radioligand.
Synthesis and Affinity Evaluation for AT1 Receptor of Phenylsalicylaldoxime-Derivatives Structurally Related to Sartans
RAPPOSELLI, SIMONA;DIGIACOMO, MARIA;LUCACCHINI, ANTONIO;MINUTOLO, FILIPPO;TRINCAVELLI, MARIA LETIZIA;
2008-01-01
Abstract
In this work we reported thy 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]Sarl,Ile8-angiotensina II as radioligand.File in questo prodotto:
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