Synthesis of [[(Benzenesulfonamido)alkyl]phenyl]alkanoic Acid Derivatives Containing Pyridyl or Imidazolyl Groups and Their Thromboxane A_2 Receptor Antagonistic and Thromboxane A_2 Synthase Inhibitory Activities
スポンサーリンク
概要
- 論文の詳細を見る
As part of our search for a dual inhibitor possessing both thromboxane A_2 (TXA_2) receptor antagonistic and TXA_2 synthase inhibitory activities, some [[(benzenesulfonamido)alkyl]phenyl]alkanoic acid derivatives possessing a pyridyl or imidazolyl group were synthesized. Their TXA_2 receptor antagonistic and TXA_2 synthase inhibitory activities were evaluated in terms of the inhibitory effects on U-44619-induced guinea-pig platelet aggregation and on thromboxane B_2 (TXB_2) production in human platelets, respectively. It was found that 3-[4-[2-(1-imidazolyl)-1-(4-chlorobenzenesulfonamido)ethyl]phenyl]propionic acid (22a), containing an imidazolyl group, is a well-balanced dual inhibitor having both TXA_2 receptor antagonistic activity (IC_<50>=0.31μM) and TXA_2 synthase inhibitory activity (IC_<50>=0.39μM).
- 公益社団法人日本薬学会の論文
- 1996-08-15
著者
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斎藤 徹
Faculty Of Pharmaceutical Sciences Kanazawa University
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YOSHIZUMI Satoshi
Kyoto Pharmaceutical University
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Yoshizumi S
Research And Development Headquaters Hokuriku Seivaku Co. Ltd.
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Kato K
Toho Univ. Chiba Jpn
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Kato K
Grad. Sch. Pharm. Sci. Nagoya City Univ.:okazaki Inst. Integ. Biosci. Natl. Inst. Natl. Sci.
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Suzuki T
Drug Discovery Research Laboratory Sanwa Kagaku Kenkyusho Co. Ltd.
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Yasuda S
Kanazawa Univ. Kanazawa Jpn
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Yasuda Shingo
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Kato H
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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Kato H
Teikyo Univ. Kanagawa Jpn
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Suzuki T
Laboratory Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Chiba University
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SAKURAI Shunichiro
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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OGAWA Nobuo
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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OHASHI Tetsuo
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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KATO Ken-ichi
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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KATO Hideo
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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SUZUKI Tomio
Research and development Division, Hokuriku Seiyaku Co., Ltd.,
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Saito Takako
Research And Development Laboratories Maruho Co. Ltd.
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Kato Ken-ichi
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Suzuki Toshikazu
Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.
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Kato Hideo
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Yasuda Satoshi
Department Of Biological Chemistry Faculty Of Pharmaceutical Sciences Nagoya City University
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Ogawa Nobuo
Department Of Biotechnology Faculty Of Engineering Osaka University
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Ogawa Nobuo
Department Of Mechanical Engineering Faculty Of Science And Technology Science University Of Tokyo
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Ohashi Tetsuo
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Ohashi Tetsuo
Research And Development Division Hokuriku Seiyaku Co. Ltd
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Suzuki T
Research Unit Of Pharmaceutics College Of Pharmacy Nihon University
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Kato Hideo
Yamaguchi Univ. Yamaguchi Jpn
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Sakurai S
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Kato Koichi
Okazaki Institute For Integrative Bioscience Institute For Molecular Science
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Ohashi T
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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