Aryl sulfonamides as selective PDE4 inhibitors

A series of novel selective phosphodiesterase 4 (PDE4) inhibitors has been developed which displays activity both in vitro and in vivo. These compounds possess good selectivity for the catalytic site of PDE4 over the high affinity Rolipram binding site. In vivo studies demonstrate a reduced propensi...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-10, Vol.8 (19), p.2635-2640
Main Authors: Montana, John G, Buckley, George M, Cooper, Nicola, Dyke, Hazel J, Gowers, Lewis, Gregory, Joanna P, Hellewell, Paul G, Kendall, Hannah J, Lowe, Christopher, Maxey, Robert, Miotla, Jadwiga, Naylor, Robert J, Runcie, Karen A, Tuladhar, Bishwa, Warneck, Julie B.H
Format: Article
Language:English
Subjects:
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:A series of novel selective phosphodiesterase 4 (PDE4) inhibitors has been developed which displays activity both in vitro and in vivo. These compounds possess good selectivity for the catalytic site of PDE4 over the high affinity Rolipram binding site. In vivo studies demonstrate a reduced propensity to display the emetic side effects which are commonly observed with PDE4 inhibitors. A series of novel selective phosphodiesterase 4 (PDE4) inhibitors, exemplified by 20, has been developed which demonstrates a good therapeutic ratio of activity against the catalytic site over the high affinity rolipram binding site of the PDE4 enzyme.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00491-0