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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1
|
| pubmed:dateCreated |
1997-3-4
|
| pubmed:abstractText |
Using the isoxazoline as a common structural feature, three series of glycoprotein IIb/IIIa receptor antagonists were evaluated, culminating in the discovery of XR299 (30). In an in vitro assay of platelet inhibition, XR299 had an IC50 of 0.24 microM and was a potent antiplatelet agent when dosed intravenously in a canine model. It was shown through X-ray studies of the cinchonidine salt 49 that the receptor required the 5(R)-stereochemistry for high potency. The ethyl ester prodrug of XR299, XR300 (29), was orally active in the dog.
|
| pubmed:commentsCorrections | |
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jan
|
| pubmed:issn |
0022-2623
|
| pubmed:author |
pubmed-author:EmmettGG,
pubmed-author:JiangBB,
pubmed-author:LiuJJ,
pubmed-author:LuMM,
pubmed-author:MousaS ASA,
pubmed-author:OlsonR ERE,
pubmed-author:PintoD JDJ,
pubmed-author:SieleckiT MTM,
pubmed-author:TobinA EAE,
pubmed-author:WangSS,
pubmed-author:WexlerR RRR,
pubmed-author:WityakJJ,
pubmed-author:ZouD YDY
|
| pubmed:issnType |
Print
|
| pubmed:day |
3
|
| pubmed:volume |
40
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
50-60
|
| pubmed:dateRevised |
2003-11-14
|
| pubmed:meshHeading | |
| pubmed:year |
1997
|
| pubmed:articleTitle |
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.
|
| pubmed:affiliation |
DuPont Merck Pharmaceutical Company, Wilmington, Delaware 19880-0500, USA.
|
| pubmed:publicationType |
Journal Article
|