A Novel Series of Thromboxane A_2 Synthetase Inhibitors with Free Radical Scavenging and Anti-peroxidative Activities
スポンサーリンク
概要
- 論文の詳細を見る
A novel series of indoline derivatives with imidazole and carboxyl moieties were synthesized and evaluated for their thromboxane A_2(TXA_2)synthetase inhibiting, radical scavenging and anti-peroxidative activities. Among the compounds synthesized, 3-{5-substituted-3-[2-(imidazol-1-yl)ethyl[indolin-1-yl}propionic acids showed free radical scavenging activity and inhibitory effects on lipid-peroxidation of rat brain homogenate and on arachidonate-induced TXA_2-dependent aggregation of rabbit platelets. The anti-platelet and anti-peroxidative activities were related to the lipophilicity of the 5-substituent. The 5-hexyloxy derivative(13)showed about 35-fold higher inhibitory activity on TXA_2 synthesis than that of ozagrel and about 100-fold higher activity on lipid peroxidation than that of α-tocopherol. Compound 13 showed in vivo anti-thrombotic effect in mice and ex vivo anti-peroxidative activity in rats.
- 公益社団法人日本薬学会の論文
- 2001-05-01
著者
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NAKAMURA Seikou
Kyoto Pharmaceutical University
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中村 紳一郎
Specialty Chemicals Research Center Shin-etsu Chemical Co. Ltd.
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Takahashi K
Faculty Of Pharmaceutical Sciences Hoshi University
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Nakamura S
Toyama Univ. Toyama Jpn
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Takahashi K
School Of Pharmaceutical Sciences Kitasato University
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Nakamura S
Specialty Chemicals Research Center Shin-etsu Chemical Co. Ltd.
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Takahashi Kenji
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd.
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Kasai Masayasu
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd.
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Kanda Mamoru
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd.
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Shirahase Hiroaki
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd.
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MATSUI Hiroshi
Research Institute for Scientific Measurements, Tohoku University
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Kanda Mamoru
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Nakamura Satoko
Osaka University Of Pharmaceutical Sciences
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Narimatsu Shizuo
Laboratories Of Health Chemistry Graduate School Of Medicine Dentistry And Pharmaceutical Sciences O
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Shirahase Hiroaki
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Shirahase Hiroaki
Research Laboratories Kyoto Pharmaceutical Company Ltd.
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Kurahashi Kazuyoshi
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Kunishiro Kazuyoshi
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Kamiya Shoji
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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NAKAMURA Shohei
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd.
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YOSHIMI Akihisa
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd.
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KURAHASHI Kazuyoshi
Pharmacology Division, Radioisotope Research Center, Kyoto University
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Kamiya S
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Nakamura Shohei
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Kanda M
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Yoshimi A
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Narimatsu Shizuo
Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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Shirahase H
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Nakamura S
Laboratories Of Health Chemistry Graduate School Of Medicine Dentistry And Pharmaceutical Sciences O
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Yoshimi Akihisa
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Kurahashi Kazuyoshi
Pharmacology Division Radioisotope Research Center And Department Of Pharmacology Faculty Of Medicin
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Matsui H
Yamaguchi Univ. Hospital Ube Jpn
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Matsui Hiroshi
Research Institute For Scientific Measurements
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Takahashi Kenji
Research And Development Group Japan Energy Corporation
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Kasai Masayasu
Research Laboratories, Kyoto Pharmaceutical Industries
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