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rdf:type |
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lifeskim:mentions |
umls-concept:C0011860,
umls-concept:C0087111,
umls-concept:C0166415,
umls-concept:C0205314,
umls-concept:C0205549,
umls-concept:C0242339,
umls-concept:C0243192,
umls-concept:C0679622,
umls-concept:C1552644,
umls-concept:C1554184,
umls-concept:C1823153,
umls-concept:C1880355,
umls-concept:C2349976
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pubmed:issue |
7
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pubmed:dateCreated |
2005-4-1
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pubmed:abstractText |
A series of 2-aryloxy-2-methyl-propionic acid compounds and related analogues were designed, synthesized, and evaluated for their PPAR agonist activities. 2-[(5,7-Dipropyl-3-trifluoromethyl)-benzisoxazol-6-yloxy]-2-methylpropionic acid (4) was identified as a PPARalpha/gamma dual agonist with relative PPARalpha selectivity and demonstrated potent efficacy in lowering both glucose and lipids in animal models without causing body weight gain. The PPARalpha activity of 4 appeared to have played a significant role in lowering glucose levels in db/db mice.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Blood Glucose,
http://linkedlifedata.com/resource/pubmed/chemical/Carrier Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Cholesterol,
http://linkedlifedata.com/resource/pubmed/chemical/Fatty Acid-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Hypoglycemic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Hypolipidemic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Isoxazoles,
http://linkedlifedata.com/resource/pubmed/chemical/PPAR alpha,
http://linkedlifedata.com/resource/pubmed/chemical/PPAR gamma,
http://linkedlifedata.com/resource/pubmed/chemical/Propionic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/RNA, Messenger,
http://linkedlifedata.com/resource/pubmed/chemical/Triglycerides
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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 |
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pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2262-5
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:15801817-3T3-L1 Cells,
pubmed-meshheading:15801817-Animals,
pubmed-meshheading:15801817-Blood Glucose,
pubmed-meshheading:15801817-COS Cells,
pubmed-meshheading:15801817-Carrier Proteins,
pubmed-meshheading:15801817-Cercopithecus aethiops,
pubmed-meshheading:15801817-Cholesterol,
pubmed-meshheading:15801817-Diabetes Mellitus, Type 2,
pubmed-meshheading:15801817-Dogs,
pubmed-meshheading:15801817-Fatty Acid-Binding Proteins,
pubmed-meshheading:15801817-Humans,
pubmed-meshheading:15801817-Hyperlipidemias,
pubmed-meshheading:15801817-Hypoglycemic Agents,
pubmed-meshheading:15801817-Hypolipidemic Agents,
pubmed-meshheading:15801817-Isoxazoles,
pubmed-meshheading:15801817-Mice,
pubmed-meshheading:15801817-Mice, Obese,
pubmed-meshheading:15801817-PPAR alpha,
pubmed-meshheading:15801817-PPAR gamma,
pubmed-meshheading:15801817-Propionic Acids,
pubmed-meshheading:15801817-RNA, Messenger,
pubmed-meshheading:15801817-Radioligand Assay,
pubmed-meshheading:15801817-Structure-Activity Relationship,
pubmed-meshheading:15801817-Transcriptional Activation,
pubmed-meshheading:15801817-Triglycerides,
pubmed-meshheading:15801817-Weight Gain
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pubmed:year |
2005
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pubmed:articleTitle |
Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
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pubmed:affiliation |
Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA. kun-liu@merck.com
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pubmed:publicationType |
Journal Article
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