Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
|
pubmed:dateCreated |
1985-10-17
|
pubmed:abstractText |
A series of new 1,3-oxazolo[4,5-h]quinolines has been prepared. These compounds were tested as inhibitors of antigen-induced release of histamine (AIR) in vitro from rat peritoneal mast cells (RMC) and as inhibitors of IgE-mediated passive cutaneous anaphylaxis in the rat (PCA). After several modifications of the original lead, the most potent compound of the series was determined to be 5-chloro-1,3-oxazolo[4,5-h]quinoline-2-carboxylic acid methyl ester (4a). It has an IC50 of 0.3 microM in the RMC assay and an ED50 (intraperitoneal) of 0.1 mg/kg in the PCA test, which is 10 times and 60 times more potent than disodium cromoglycate (DSCG), respectively. Of greater importance, it is orally active (ED50 = 0.5 mg/kg) as an inhibitor of the PCA test.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Sep
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
28
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1255-9
|
pubmed:dateRevised |
2008-11-21
|
pubmed:meshHeading |
pubmed-meshheading:2411926-Animals,
pubmed-meshheading:2411926-Chemical Phenomena,
pubmed-meshheading:2411926-Chemistry,
pubmed-meshheading:2411926-Cromolyn Sodium,
pubmed-meshheading:2411926-Histamine Release,
pubmed-meshheading:2411926-Immunoglobulin E,
pubmed-meshheading:2411926-Mast Cells,
pubmed-meshheading:2411926-Oxazoles,
pubmed-meshheading:2411926-Passive Cutaneous Anaphylaxis,
pubmed-meshheading:2411926-Quinolines,
pubmed-meshheading:2411926-Rats,
pubmed-meshheading:2411926-Structure-Activity Relationship
|
pubmed:year |
1985
|
pubmed:articleTitle |
Synthesis and antiallergic activities of 1,3-oxazolo[4,5-h]quinolines.
|
pubmed:publicationType |
Journal Article,
Comparative Study
|