嘧啶基吡咯并喹诺酮类化合物作为治疗勃起功能障碍的高效且选择性的磷酸二酯酶5抑制剂。

Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.

作者信息

Sui Zhihua, Guan Jihua, Macielag Mark J, Jiang Weiqin, Zhang Suying, Qiu Yuhong, Kraft Patricia, Bhattacharjee Sheela, John T Matthew, Haynes-Johnson Donna, Clancy Joanna

机构信息

Johnson & Johnson Pharmaceutical Research & Development, Drug Discovery, 1000 Route 202, Raritan, NJ 08869, USA.

出版信息

J Med Chem. 2002 Sep 12;45(19):4094-6. doi: 10.1021/jm025545d.

DOI:10.1021/jm025545d

PMID:12213052

Abstract

A series of N-pyrimidinylpyrroloquinolones were discovered as extremely potent and selective PDE5 inhibitors. Representative compounds demonstrated in vivo efficacy in dog erectile dysfunction models and are orally bioavailable.

摘要

一系列N-嘧啶基吡咯并喹诺酮被发现是极其强效且具有选择性的磷酸二酯酶5（PDE5）抑制剂。代表性化合物在犬勃起功能障碍模型中显示出体内疗效，并且口服具有生物利用度。