Source:http://linkedlifedata.com/resource/pubmed/id/12699396
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
9
|
| pubmed:dateCreated |
2003-4-17
|
| pubmed:abstractText |
SAR studies of 7-phenylpyrrolo[1,2-a]pyrimid-4-ones 1 and 2, and 2-phenylimidazolo[1,2-a]pyrimidines 3 and 4, as nonpeptide human GnRH receptor antagonists, lead us to believe that the aromatic ring at position-2 of 4 is no longer crucial for the binding once an aryl group is incorporated at postion-6. We report here the use of a 2-alkyl group on the imidazolo[1,2-a]pyrimidone core to generate potent GnRH receptor antagonists. This discovery enabled us to obtain smaller but equally potent GnRH receptor antagonists.
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| pubmed:grant | |
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Apr
|
| pubmed:issn |
0022-2623
|
| pubmed:author |
pubmed-author:ConnorsPatrick JPJJr,
pubmed-author:GaoYinghongY,
pubmed-author:GrossTimothy DTD,
pubmed-author:GuoZhiqiangZ,
pubmed-author:ReinhartGreg JGJ,
pubmed-author:SaundersJohnJ,
pubmed-author:StruthersR ScottRS,
pubmed-author:TucciFabio CFC,
pubmed-author:WuDongpeiD,
pubmed-author:XXX,
pubmed-author:YewP RPR,
pubmed-author:ZhuYun-FeiYF
|
| pubmed:issnType |
Print
|
| pubmed:day |
24
|
| pubmed:volume |
46
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1769-72
|
| pubmed:dateRevised |
2007-11-14
|
| pubmed:meshHeading | |
| pubmed:year |
2003
|
| pubmed:articleTitle |
Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
|
| pubmed:affiliation |
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 10555 Science Center Drive, San Diego, California 92121, USA.
|
| pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
|