rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
10
|
pubmed:dateCreated |
1997-6-6
|
pubmed:abstractText |
A series of 6-aryl-4,5-heterocyclic-fused pyridazinones were designed and synthesized as selective phosphodiesterase (PDE) IV inhibitors. Biological evaluation of these compounds demonstrated a good selectivity profile toward the PDE IV family and greatly attenuated affinity for the Rolipram high-affinity binding site that seems to be responsible for undesiderable side effects. Structure-activity relationships (SARs) studies showed that the presence of an ethyl group at pyridazine N-2 is associated with the best potency and selectivity profile.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0022-2623
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
9
|
pubmed:volume |
40
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1417-21
|
pubmed:dateRevised |
2007-11-15
|
pubmed:meshHeading |
pubmed-meshheading:9154964-3',5'-Cyclic-AMP Phosphodiesterases,
pubmed-meshheading:9154964-Animals,
pubmed-meshheading:9154964-Brain,
pubmed-meshheading:9154964-Cyclic Nucleotide Phosphodiesterases, Type 4,
pubmed-meshheading:9154964-Enzyme Inhibitors,
pubmed-meshheading:9154964-Guinea Pigs,
pubmed-meshheading:9154964-Magnetic Resonance Spectroscopy,
pubmed-meshheading:9154964-Phosphoric Diester Hydrolases,
pubmed-meshheading:9154964-Pyridazines,
pubmed-meshheading:9154964-Pyrrolidinones,
pubmed-meshheading:9154964-Radioligand Assay,
pubmed-meshheading:9154964-Rats,
pubmed-meshheading:9154964-Rolipram,
pubmed-meshheading:9154964-Structure-Activity Relationship
|
pubmed:year |
1997
|
pubmed:articleTitle |
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.
|
pubmed:affiliation |
Dipartimento di Scienze Farmaceutiche, Firenze, Italy.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|