The discovery of novel, potent and selective PDE5 inhibitors

Authors
Bi, YZ Stoy, P Adam, L He, B Krupinski, J Normandin, D Pongrac, R Seliger, L Watson, A Macor, JE
Citation
Yz. Bi et al., The discovery of novel, potent and selective PDE5 inhibitors, BIOORG MED, 11(18), 2001, pp. 2461-2464
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
18
Year of publication
2001
Pages
2461 - 2464
Database
ISI
SICI code
0960-894X(20010917)11:18<2461:TDONPA>2.0.ZU;2-V
Abstract
The design and synthesis of a novel scaffold for potent and selective PDE5 inhibitors are described. Compound 3a was more potent (PDE5 IC50 = 0.31 nM) and selective (> 10,000-fold vs PDE1 and 160-fold selective vs PDE6) PDE5 inhibitor than sildenafil. (C) 2001 Elsevier Science Ltd. All rights reserv ed.