Studies on Non-Thiazolidinedione Antidiabetic Agents. 3. Preparation and Biological Activity of the Metabolites of TAK-559
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概要
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Preparation and biological activity of the metabolites of the potent antihyperglycemic and antihyperlipidemic agent, (E)-4-{4-[(5-methyl-2-phenyl-1,3-oxazol-4-yl)methoxy]benzyloxyimino}-4-phenylbutyric acid (TAK-559) (1), were investigated. Metabolites M-I (2), M-II (3), M-III (4) and M-IV (5) were synthesized and their biological activities were evaluated by in vitro and in vivo experiments. Compounds 2-4 activate human peroxisome proliferator-activated receptor gamma one (hPPARγ1) and hPPARα, but their activities are weaker than those of TAK-559 (1). Compound 5 only activates hPPARγ1 weakly. TAK-559 (1) showed potent in vivo plasma glucose and triglyceride lowering activities in Wistar fatty rats after intraperitoneal administration, while its metabolites (2-5) showed comparatively weak activities.
- 公益社団法人日本薬学会の論文
- 2004-01-01
著者
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Matsumoto M
Osaka Medical Center For Cancer And Cardiovascular Diseases Osaka
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Matsumoto Misako
Department Of Immunology Osaka Medical Center For Cancer And Cardiovascular Diseases
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Kiyota Y
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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Kiyota Yutaka
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
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Matsumoto Mitsuharu
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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Imoto Hiroshi
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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Odaka H
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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ODAKA Hiroyuki
Takeda Chemical Industries, Ltd. Pharmaceutical Research Division
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NONAKA Masami
Takeda Chemical Industries, Ltd. Pharmaceutical Research Division
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KIYOTA Yutaka
Takeda Chemical Industries, Ltd. Pharmaceutical Research Division
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MOMOSE Yu
Takeda Chemical Industries, Ltd. Pharmaceutical Research Division
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Momose Yu
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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Nonaka Masami
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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Matsumoto Mitsuhiro
First Department Of Internal Medicine Kumamoto University School Of Medicine
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