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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
2011-5-20
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pubmed:abstractText |
The discovery of novel and highly potent oxopiperazine based B1 receptor antagonists is described. Compared to the previously described arylsulfonylated (R)-3-amino-3-phenylpropionic acid series, the current compounds showed improved in vitro potency and metabolic stability. Compound 17, 2-((2R)-1-((4-methylphenyl)sulfonyl)-3-oxo-2-piperazinyl)-N-((1R)-6-(1-piperidinylmethyl)-1,2,3,4-tetrahydro-1-naphthalenyl)acetamide, showed EC(50) of 10.3 nM in a rabbit biochemical challenge model. The practical syntheses of chiral arylsulfonylated oxopiperazine acetic acids are also described.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AndersenNeil GNG,
pubmed-author:AskewBenny CBC,
pubmed-author:AyaToshihiroT,
pubmed-author:BiswasKaustavK,
pubmed-author:ChenJian JeffreyJJ,
pubmed-author:ColyerJohn TJT,
pubmed-author:D'AmicoDerin CDC,
pubmed-author:FaulMargaret MMM,
pubmed-author:FotschChristopherC,
pubmed-author:HanNianheN,
pubmed-author:HumanJasonJ,
pubmed-author:HungateRandall WRW,
pubmed-author:JohnsonEileenE,
pubmed-author:JonaJananJ,
pubmed-author:KamassahAugustusA,
pubmed-author:KumarGondiG,
pubmed-author:LiuQingyianQ,
pubmed-author:NguyenThomasT,
pubmed-author:NishimuraNobukoN,
pubmed-author:PeterkinTanya A NTA,
pubmed-author:QianWenyuanW,
pubmed-author:RiahiBabak BobbyBB,
pubmed-author:WangJudyJ,
pubmed-author:YangKevinK,
pubmed-author:ZhuJiawangJ
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pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3384-9
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pubmed:meshHeading |
pubmed-meshheading:21514825-Acetamides,
pubmed-meshheading:21514825-Animals,
pubmed-meshheading:21514825-Dogs,
pubmed-meshheading:21514825-Inflammation,
pubmed-meshheading:21514825-Inhibitory Concentration 50,
pubmed-meshheading:21514825-Mice,
pubmed-meshheading:21514825-Models, Animal,
pubmed-meshheading:21514825-Molecular Structure,
pubmed-meshheading:21514825-Pain,
pubmed-meshheading:21514825-Piperazines,
pubmed-meshheading:21514825-Rabbits,
pubmed-meshheading:21514825-Rats,
pubmed-meshheading:21514825-Receptor, Bradykinin B1,
pubmed-meshheading:21514825-Stereoisomerism,
pubmed-meshheading:21514825-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation.
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pubmed:affiliation |
Department of Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States. jianc@amgen.com
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pubmed:publicationType |
Journal Article
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