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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2010-2-22
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pubmed:abstractText |
Elevated stearoyl-CoA desaturase (SCD) activity has been linked to a number of metabolic disorders including obesity and type II diabetes. Compound 3j, a potent SCD inhibitor (human HepG2 IC(50)=1nM) was identified from the optimization of a lead thiazole compound MF-152 with over 100-fold improvement in potency. In a 4-week chronic oral dosing at 0.2mg/kg, 3j gave a robust 24% prevention of body weight gain in mice fed on a high fat diet accompanied with an improved metabolic profile on insulin and glucose levels.
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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 |
Mar
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BlackCameronC,
pubmed-author:ChanChi-ChungCC,
pubmed-author:CraneSheldonS,
pubmed-author:GuayJocelyneJ,
pubmed-author:GuiralSébastienS,
pubmed-author:HuangZhengZ,
pubmed-author:LiChun SingCS,
pubmed-author:OballaRenataR,
pubmed-author:RamtohulYeeman KYK,
pubmed-author:XuLi-JingLJ,
pubmed-author:ZhangLeiL
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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 |
1
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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 |
1593-7
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pubmed:meshHeading |
pubmed-meshheading:20137926-Administration, Oral,
pubmed-meshheading:20137926-Animals,
pubmed-meshheading:20137926-Dietary Fats,
pubmed-meshheading:20137926-Enzyme Inhibitors,
pubmed-meshheading:20137926-Hep G2 Cells,
pubmed-meshheading:20137926-Humans,
pubmed-meshheading:20137926-Hypoglycemic Agents,
pubmed-meshheading:20137926-Mice,
pubmed-meshheading:20137926-Mice, Inbred C57BL,
pubmed-meshheading:20137926-Oxadiazoles,
pubmed-meshheading:20137926-Stearoyl-CoA Desaturase,
pubmed-meshheading:20137926-Structure-Activity Relationship,
pubmed-meshheading:20137926-Thiazoles,
pubmed-meshheading:20137926-Weight Gain
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pubmed:year |
2010
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pubmed:articleTitle |
SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, 16711 TransCanada Hwy, Kirkland, Quebec, Canada H9H 3L1. yeeman_ramtohul@merck.com
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pubmed:publicationType |
Journal Article
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