Synthesis and biological evaluation of 2,5-dihydropyrazolo[4,3-c]quinolin-3-ones, a novel series of PDE 4 inhibitors with low emetic potential and antiasthmatic properties

Authors
Crespo, MI Gracia, J Puig, C Vega, A Bou, J Beleta, J Domenech, T Ryder, H Segarra, V Palacios, JM
Citation
Mi. Crespo et al., Synthesis and biological evaluation of 2,5-dihydropyrazolo[4,3-c]quinolin-3-ones, a novel series of PDE 4 inhibitors with low emetic potential and antiasthmatic properties, BIOORG MED, 10(23), 2000, pp. 2661-2664
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
23
Year of publication
2000
Pages
2661 - 2664
Database
ISI
SICI code
0960-894X(200012)10:23<2661:SABEO2>2.0.ZU;2-G
Abstract
A novel series of 2,5-dihydropyrazolo[4,3-c]quinolin-3-one has been prepare d. These compounds showed good PDE 4 inhibitory activity and weak affinity for rolipram's binding site. They also exhibited a good anti-inflammatory p rofile without emetic side effects. (C) 2000 Published by Elsevier Science Ltd.