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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2007-4-12
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pubmed:abstractText |
Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the levels of active glucagon-like peptide-1 and glucose-dependent insulinotropic peptide, which are two important incretins for glucose homeostasis. Starting from a high-throughput screening hit, we were able to identify a series of piperidinone- and piperidine-constrained phenethylamines as novel DPP4 inhibitors. Optimized compounds are potent, selective, and have good pharmacokinetic profiles.
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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 |
0022-2623
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pubmed:author |
pubmed-author:BackesBradley JBJ,
pubmed-author:BallaronStephen JSJ,
pubmed-author:BenoDavid W ADW,
pubmed-author:Kempf-GroteAnita JAJ,
pubmed-author:LaiChunqiuC,
pubmed-author:LiXiaofengX,
pubmed-author:LongeneckerKentonK,
pubmed-author:LubbenThomas HTH,
pubmed-author:PeiZhonghuaZ,
pubmed-author:PirehDaisyD,
pubmed-author:ShamHing LHL,
pubmed-author:StewartKent DKD,
pubmed-author:TrevillyanJames MJM,
pubmed-author:von GeldernThomas WTW
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pubmed:issnType |
Print
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pubmed:day |
19
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1983-7
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:17367123-Adenosine Deaminase Inhibitors,
pubmed-meshheading:17367123-Animals,
pubmed-meshheading:17367123-Biological Availability,
pubmed-meshheading:17367123-Crystallography, X-Ray,
pubmed-meshheading:17367123-Dipeptidyl Peptidase 4,
pubmed-meshheading:17367123-Dipeptidyl-Peptidase IV Inhibitors,
pubmed-meshheading:17367123-Glycoproteins,
pubmed-meshheading:17367123-Humans,
pubmed-meshheading:17367123-Molecular Conformation,
pubmed-meshheading:17367123-Phenethylamines,
pubmed-meshheading:17367123-Piperidines,
pubmed-meshheading:17367123-Piperidones,
pubmed-meshheading:17367123-Rats,
pubmed-meshheading:17367123-Stereoisomerism,
pubmed-meshheading:17367123-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
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pubmed:affiliation |
Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-3500, USA. zhonghua.pei@abbott.com
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pubmed:publicationType |
Journal Article
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