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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
2010-6-4
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pubmed:abstractText |
A series of carboxylic acid glycogen phosphorylase inhibitors, which have potential as oral antidiabetic agents, is described. Defining and applying simple physicochemical design criteria was used to assess the opportunity and to focus synthetic efforts on compounds with the greatest probability of success. The study led to compound 17, which exhibits a good balance of properties including potent inhibition of recombinant human liver glycogen phosphorylase in vitro, a good DMPK profile including excellent bioavailability and low clearance and good in vivo activity in a glucagon challenge model of diabetes in Zucker rats.
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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:BennettStuart N LSN,
pubmed-author:CampbellAndrew DAD,
pubmed-author:HancockAndrewA,
pubmed-author:JohnstoneCraigC,
pubmed-author:KennyPeter WPW,
pubmed-author:PickupAdrianA,
pubmed-author:PlowrightAlleyn TAT,
pubmed-author:SelmiNidhalN,
pubmed-author:SimpsonIainI,
pubmed-author:StockerAndyA,
pubmed-author:WhalleyDavid PDP,
pubmed-author:WhittamorePaul R OPR
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3511-4
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pubmed:meshHeading |
pubmed-meshheading:20493691-Animals,
pubmed-meshheading:20493691-Biological Availability,
pubmed-meshheading:20493691-Carboxylic Acids,
pubmed-meshheading:20493691-Drug Discovery,
pubmed-meshheading:20493691-Glycogen Phosphorylase, Liver Form,
pubmed-meshheading:20493691-Humans,
pubmed-meshheading:20493691-Hypoglycemic Agents,
pubmed-meshheading:20493691-Indans,
pubmed-meshheading:20493691-Rats,
pubmed-meshheading:20493691-Rats, Zucker
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pubmed:year |
2010
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pubmed:articleTitle |
Discovery of a series of indan carboxylic acid glycogen phosphorylase inhibitors.
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pubmed:affiliation |
AstraZeneca, Medicinal Chemistry, Cardiovascular and Gastrointestinal Research Area, Alderley Park, Macclesfield, Cheshire, UK.
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pubmed:publicationType |
Journal Article
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