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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
21
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pubmed:dateCreated |
2007-10-11
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pubmed:abstractText |
The B1 receptor is an attractive target for the treatment of pain and inflammation. A series of 3-carboxamido-5-phenacylamino pyrazole B1 receptor antagonists are described that exhibit good potency against B1 and high selectivity over B2. Initially, N-unsubstituted pyrazoles were studied, but these compounds suffered from extensive glucuronidation in primates. This difficulty could be surmounted by the use of N-substituted pyrazoles. Optimization efforts culminated in compound 41, which has high receptor potency and metabolic stability.
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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 |
Oct
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:DressenDarrenD,
pubmed-author:GarofaloAlbert WAW,
pubmed-author:HawkinsonJonJ,
pubmed-author:HomDennisD,
pubmed-author:JagodzinskiJacekJ,
pubmed-author:MaruggJennifer LJL,
pubmed-author:NeitzelMartin LML,
pubmed-author:PleissMichael AMA,
pubmed-author:SzokeBalazsB,
pubmed-author:TungJay SJS,
pubmed-author:WoneDavid W GDW,
pubmed-author:WuJingJ,
pubmed-author:ZhangHeatherH
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pubmed:issnType |
Print
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pubmed:day |
18
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pubmed:volume |
50
|
|
pubmed:owner |
NLM
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|
pubmed:authorsComplete |
Y
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pubmed:pagination |
5161-7
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pubmed:meshHeading |
pubmed-meshheading:17880055-Benzamides,
pubmed-meshheading:17880055-Crystallography, X-Ray,
pubmed-meshheading:17880055-Fibroblasts,
pubmed-meshheading:17880055-Humans,
pubmed-meshheading:17880055-Lung,
pubmed-meshheading:17880055-Molecular Structure,
pubmed-meshheading:17880055-Pyrazoles,
pubmed-meshheading:17880055-Radioligand Assay,
pubmed-meshheading:17880055-Receptor, Bradykinin B1,
pubmed-meshheading:17880055-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.
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pubmed:affiliation |
Elan Pharmaceuticals, Inc., 800 Gateway Boulevard, South San Francisco, California 94080, USA. al.garofalo@elan.com
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pubmed:publicationType |
Journal Article,
In Vitro
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