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化学学报
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化学学报 ›› 2007, Vol. 65 ›› Issue (24): 2917-2922. 上一篇    下一篇

研究论文

伐地那非衍生物的合成和体内活性评价

王进欣1,2, 储刚1, 孙飘扬*,2, 周福强2, 尤启冬*,1   

  1. (1中国药科大学药物化学教研室 南京 210009)
    (2江苏恒瑞制药股份有限公司 连云港 222002)
  • 投稿日期:2006-09-11 修回日期:2007-04-12 发布日期:2007-12-28
  • 通讯作者: 尤启冬

Synthesis of Vardenafil Analogue and Its Activity Evaluation in vivo

WANG Jin-Xin1,2; CHU Gang1; SUN Piao-Yang*,2; ZHOU Fu-Qiang2; YOU Qi-Dong*,1   

  1. (1 Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009)
    (2 Jiangsu Hengrui Pharmaceutical Company, Lianyungang 222002)
  • Received:2006-09-11 Revised:2007-04-12 Published:2007-12-28
  • Contact: YOU Qi-Dong

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首次完成了伐地那非衍生物—2-[2-乙氧基-5-(4-乙基-哌嗪-1-磺酰基)-吡啶]-5-甲基-7-丙基-3H-咪唑[5,1-f]-三 嗪-4-酮(1)的合成, 并且对其进行了家兔阴茎勃起的体内实验, 结果表明该化合物无壮阳作用.

关键词: 磷酸二酯酶5抑制剂, 伐地那非, 咪唑并三嗪, 男性勃起功能障碍

The first synthesis of a Vardenafil analogue 1-methyl-3-prepyl-5-[2-[2-ethoxy-5-(4-ethyl piperazinosulfonyl)-3-pyridyl]-6H-imidazo[1,5-f]-1',2',4'-triazin-7-one (1) was achieved, and compound 1 was evaluated by the erections in rabbits in vivo which exhibited no potency to the treatment of erectile dysfunction.

Key words: phosphodiesterase 5 inhibitor, vardenafil, imidazotriazine, male erectile dysfunction