Abstract
The syntheses and in vitro evaluation of a new series of pyrido[2,3-d]pyrimidine-2,4-diones bearing substituents at C-3 and/or C-4 positions on the pyridine ring are described. Some of these compounds, especially 51 and 6f, were found to be potent phosphodiesterase 4 (PDE 4) inhibitors exhibiting improved ratio of PDE 4 inhibitory activity:rolipram binding assay (RBA).
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
-
3',5'-Cyclic-AMP Phosphodiesterases / metabolism
-
Animals
-
Biological Assay
-
Cyclic Nucleotide Phosphodiesterases, Type 4
-
Humans
-
Molecular Structure
-
Phosphodiesterase Inhibitors / chemical synthesis*
-
Phosphodiesterase Inhibitors / chemistry
-
Phosphodiesterase Inhibitors / pharmacology*
-
Pyrimidines / chemical synthesis*
-
Pyrimidines / chemistry
-
Pyrimidines / metabolism
-
Pyrimidines / pharmacology*
-
Quinazolines / chemical synthesis*
-
Quinazolines / chemistry*
-
Quinazolines / pharmacology*
-
Rats
-
Rolipram / metabolism
Substances
-
CP 77059
-
Phosphodiesterase Inhibitors
-
Pyrimidines
-
Quinazolines
-
RS 25344
-
3',5'-Cyclic-AMP Phosphodiesterases
-
Cyclic Nucleotide Phosphodiesterases, Type 4
-
Rolipram