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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2009-3-16
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pubmed:abstractText |
A series of 4-substituted proline amides was synthesized and evaluated as inhibitors of dipeptidyl pepdidase IV for the treatment of type 2 diabetes. (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone (5) emerged as a potent (IC(50) = 13 nM) and selective compound, with high oral bioavailability in preclinical species and low plasma protein binding. Compound 5, PF-00734200, was selected for development as a potential new treatment for type 2 diabetes.
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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 |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AmmiratiMark JMJ,
pubmed-author:AndrewsKim MKM,
pubmed-author:BoyerDavid DDD,
pubmed-author:BrodeurAnne MAM,
pubmed-author:DanleyDennis EDE,
pubmed-author:DoranShawn DSD,
pubmed-author:HulinBernardB,
pubmed-author:LiuShenpingS,
pubmed-author:McPhersonR KirkRK,
pubmed-author:OrenaStephen JSJ,
pubmed-author:ParkerJanice CJC,
pubmed-author:PiotrowskiDavid WDW,
pubmed-author:PolivkovaJanaJ,
pubmed-author:QiuXiayangX,
pubmed-author:SogliaCarolyn BCB,
pubmed-author:TreadwayJudith LJL,
pubmed-author:VanVolkenburgMaria AMA,
pubmed-author:WilderDonald CDC
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1991-5
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pubmed:meshHeading |
pubmed-meshheading:19275964-Administration, Oral,
pubmed-meshheading:19275964-Animals,
pubmed-meshheading:19275964-Crystallography, X-Ray,
pubmed-meshheading:19275964-Diabetes Mellitus, Type 2,
pubmed-meshheading:19275964-Dipeptidyl-Peptidase IV Inhibitors,
pubmed-meshheading:19275964-Dogs,
pubmed-meshheading:19275964-Humans,
pubmed-meshheading:19275964-Hypoglycemic Agents,
pubmed-meshheading:19275964-Pyrimidines,
pubmed-meshheading:19275964-Pyrrolidines,
pubmed-meshheading:19275964-Rats,
pubmed-meshheading:19275964-Rats, Sprague-Dawley,
pubmed-meshheading:19275964-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.
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pubmed:affiliation |
Pfizer Global Research & Development, Groton/New London Laboratories, Pfizer Inc, Groton, CT 06340, United States.
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pubmed:publicationType |
Journal Article
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