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1. Synthesis and Affinity Evaluation for AT1 Receptor of Phenylsalicylaldoxime-Derivatives Structurally Related to Sartans

Author

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

Subjects
Pharmacology, Angiotensin II receptor type 1, Stereochemistry, Ligand binding assay, Organic Chemistry, Salicylaldoxime, Analytical Chemistry, chemistry.chemical_compound, Membrane, Losartan, chemistry, Rat liver, Radioligand, medicine, hormones, hormone substitutes, and hormone antagonists, medicine.drug
Abstract

In this work we reported the synthesis of new potential ATI 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 [ 125 I]Sar1,Ile8-angiotensina II as radioligand.

Published
2008
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