Synthesis and pharmacological evaluation of new pyrazolidine-3, 5-diones as AT1 angiotensin II receptor antagonists

B Le Bourdonnec, E Meulon, S Yous…

Index: Le Bourdonnec, Bertrand; Meulon, Emmanuelle; Yous, Said; Goossens, Jean-Francois; Houssin, Raymond; Henichart, Jean-Pierre Journal of Medicinal Chemistry, 2000 , vol. 43, # 14 p. 2685 - 2697

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Citation Number: 54

Abstract

On the basis of the structure of the non-peptide receptor antagonist irbesartan, a new series of AT1 ligands was designed. In these compounds the central imidazolone nucleus of irbesartan was replaced by a pyrazolidine-3, 5-dione structure. The key intermediate N- alkylpyrazolidine-3, 5-diones were synthesized according to a new and general method. The most active compounds possess a spirocyclopentane ring at position 4, a linear butyl ...

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