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...
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Published in: | Bioorganic & medicinal chemistry letters 1998-10, Vol.8 (19), p.2635-2640 |
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Main Authors: | , , , , , , , , , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(98)00491-0 |