Studies on Disease-Modifying Antirheumatic Drugs. III. Bone Resorption Inhibitory Effects of Ethyl 4-(3,4-Dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4-triazol-1-ylmethyl)quinoline-3-carboxylate (TAK-603) and Related Compounds
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概要
- 論文の詳細を見る
In the course of our studies aimed at obtaining new drugs for treatment of bone and joint diseases, chemical modification of the potent bone resorption inhibitors justicidins, was performed and various naphthalene lactones, quinoline lactones and quinoline derivatives bearing an azole moiety at the side chain were prepared. Their inhibitory effects on bone resorption were evaluated by Raisz's method, and several compounds, including ethyl 4-(3,4-dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4-triazol-1-ylmethyl)quinoline-3-carboxylate (6c, TAK-603), were found to have activities comparable with or superior to the justicidins. The 4-(3-isopropoxy-4-methoxy)-phenyl derivative (6d), in particular, displayed a marked increase in potency. TAK-603 and compound 6d were very effective in preventing osteoclast formation and bone resorption by mature osteoclasts. Further, TAK-603 was shown to be effective in preventing bone loss in ovariectomized mice.
- 公益社団法人日本薬学会の論文
- 1999-03-15
著者
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左右田 隆
武田薬品工業株式会社医薬研究本部
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Oda Tsuneo
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
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Notoya Kohei
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
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Sohda T
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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TAKETOMI Shigehisa
Pharmaceutical Research Laboratories II, Takeda Chemical Industries, Ltd.
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Makino H
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
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Notoya K
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
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BABA Atsuo
Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
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NISHIMURA Atsushi
Discovery Research Division, Takeda Chemical Industries, Ltd.,
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MAKINO Haruhiko
Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
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SOHDA Takashi
Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
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Taketomi S
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
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Taketomi Shigehisa
Pharmaceutical Research Laboratories Ii Takeda Chemical Industries Ltd.
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Baba A
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
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Nishimura Atsushi
Discovery Research Division Takeda Chemical Industries Ltd.
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Taketomi Shigehisa
Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
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