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Synthesis and pharmacological evaluations of sildenafil analogues for treatment of erectile dysfunction

…, B Severino, F Frecentese, R Lorenzetti…

文献索引:Flores Toque, Haroldo A.; Priviero, Fernanda B. M.; Teixeira, Cleber E.; Perissutti, Elisa; Fiorino, Ferdinando; Severino, Beatrice; Frecentese, Francesco; Lorenzetti, Raquel; Baracat, Juliana S.; Santagada, Vincenzo; Caliendo, Giuseppe; Antunes, Edson; De Nucci, Gilberto Journal of Medicinal Chemistry, 2008 , vol. 51, # 9 p. 2807 - 2815

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被引用次数: 28

摘要

The 5-[2-ethoxy-5-(4-methylpiperazin-1-ylsulfonyl) phenyl]-1-methyl-3-propyl-1, 6-dihydro-7 H-pyrazolo [4, 3-d] pyrimidin-7-one, sildenafil, is a cGMP-specific phosphodiesterase-5 (PDE5) inhibitor used for penile erectile dysfunction. In the search for more potent and selective PDE5 inhibitors, new sildenafil analogues (6a− v), characterized by the presence on the sulfonyl group in the 5′ position of novel N-4-substituted piperazines or ...