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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2000-9-8
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pubmed:abstractText |
A series of imidazopyridine thiazolidine-2,4-diones were designed and synthesized from their corresponding pyridines. These compounds represent conformationally restricted analogues of the novel hypoglycemic compound rosiglitazone (5). The series was evaluated for its effect on insulin-induced 3T3-L1 adipocyte differentiation in vitro and its hypoglycemic activity in the genetically diabetic KK mouse in vivo. The structure-activity relationships are discussed. On the basis of the in vivo potency, 5-[4-(5-methoxy-3-methyl-3H-imidazo[4, 5-b]pyridin-2-ylmethoxy)benzyl]thiazolidine-2,4-dione (19a) was selected as the candidate for further studies in a clinical setting.
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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 |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:FujitaTT,
pubmed-author:FujiwaraTT,
pubmed-author:HonmaHH,
pubmed-author:HorikoshiHH,
pubmed-author:KanekoTT,
pubmed-author:OguchiMM,
pubmed-author:OhsumiJJ,
pubmed-author:SakakibaraSS,
pubmed-author:SerizawaNN,
pubmed-author:TanakaAA,
pubmed-author:WadaKK
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pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
43
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3052-66
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:10956213-3T3 Cells,
pubmed-meshheading:10956213-Adipocytes,
pubmed-meshheading:10956213-Animals,
pubmed-meshheading:10956213-Biological Availability,
pubmed-meshheading:10956213-Cell Differentiation,
pubmed-meshheading:10956213-Diabetes Mellitus,
pubmed-meshheading:10956213-Drug Design,
pubmed-meshheading:10956213-Drug Evaluation, Preclinical,
pubmed-meshheading:10956213-Heart,
pubmed-meshheading:10956213-Hypoglycemic Agents,
pubmed-meshheading:10956213-Imidazoles,
pubmed-meshheading:10956213-Male,
pubmed-meshheading:10956213-Mice,
pubmed-meshheading:10956213-Organ Size,
pubmed-meshheading:10956213-Rats,
pubmed-meshheading:10956213-Structure-Activity Relationship,
pubmed-meshheading:10956213-Thiazoles,
pubmed-meshheading:10956213-Thiazolidinediones
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pubmed:year |
2000
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pubmed:articleTitle |
Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones.
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pubmed:affiliation |
Medicinal Chemistry Research Laboratories, Sankyo Company, Ltd., 2-58 Hiromachi 1-chome, Shinagawa-ku, Tokyo 140-8710, Japan. oguchi@shina.sankyo.co.jp
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pubmed:publicationType |
Journal Article
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