Potent and selective xanthine-based inhibitors of phosphodiesterase 5

被引：13

作者：

Arnold, Nichola J.

Arnold, Ruth

Beer, David

Bhalay, Gurdip

Collingwood, Stephen P.

Craig, Sarah

Devereux, Nicholas

Dodds, Mark

Dunstan, Andrew R.

Fairhurst, Robin A.

Farr, David

Fullerton, Joseph D.

Glen, Angela

Gomez, Sylvie

Haberthuer, Sandra

Hatto, Julia D. I.

Howes, Colin

Jones, Darryl

Keller, Thomas H.

Leuenberger, Beate

Moser, Heinz E.

Muller, Irene

Naef, Reto

Nicklin, Paul A.

Sandham, David A.

Turner, Katharine L.

Tweed, Morris F.

Watson, Simon J.

Zurini, Mauro

机构：

[1] Horsham Res Ctr, Novartis Inst Biomed Res, Horsham RH12 5AB, W Sussex, England

[2] Novartis Inst Biomed Res, CH-4056 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 08期

关键词：

phosphodiesterase; 5; xanthine; erectile dysfunction;

D O I：

10.1016/j.bmcl.2006.11.019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibitors of PDE5 are useful therapeutic agents for treatment of erectile dysfunction. A series of novel xanthine derivatives has been identified as potent inhibitors of PDE5, with good levels of selectivity against other PDE isoforms, including PDE6. Studies in the dog indicate excellent oral bioavailability for compound 21. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2376 / 2379

页数：4

共 20 条

[1] 8-aryl xanthines potent inhibitors of phosphodiesterase 5 [J].