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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2007-11-16
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pubmed:abstractText |
The cis-3-amino-4-(2-cyanopyrrolidide)-pyrrolidine template has been shown to afford low nanomolar inhibitors of human DPP-IV that exhibit a robust PK/PD profile. An X-ray co-crystal structure of 5 confirmed the proposed mode of binding. The potent single digit DPP-IV inhibitor 53 exhibited a preferred PK/PD profile in preclinical animal models and was selected for additional profiling.
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pubmed:commentsCorrections |
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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 |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AmmiratiMM,
pubmed-author:BoscoeB PBP,
pubmed-author:BoyetFF,
pubmed-author:CorbettJ WJW,
pubmed-author:DiricoKK,
pubmed-author:DoranS DSD,
pubmed-author:HouH CHC,
pubmed-author:McPhersonR KRK,
pubmed-author:ParkerJ CJC,
pubmed-author:QinSS,
pubmed-author:SongWW,
pubmed-author:VanvolkenburgM AMA
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6707-13
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:17977724-Amination,
pubmed-meshheading:17977724-Animals,
pubmed-meshheading:17977724-Benzene,
pubmed-meshheading:17977724-Cyanides,
pubmed-meshheading:17977724-Dipeptidyl Peptidase 4,
pubmed-meshheading:17977724-Dipeptidyl-Peptidase IV Inhibitors,
pubmed-meshheading:17977724-Dogs,
pubmed-meshheading:17977724-Drug Design,
pubmed-meshheading:17977724-Humans,
pubmed-meshheading:17977724-Inhibitory Concentration 50,
pubmed-meshheading:17977724-Models, Molecular,
pubmed-meshheading:17977724-Molecular Structure,
pubmed-meshheading:17977724-Protease Inhibitors,
pubmed-meshheading:17977724-Pyrroles,
pubmed-meshheading:17977724-Rats,
pubmed-meshheading:17977724-Stereoisomerism,
pubmed-meshheading:17977724-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors.
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pubmed:affiliation |
Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA.
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pubmed:publicationType |
Journal Article
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