Synthesis and Dual Antagonistic Activity against Thromboxane A_2 and Leukotriene D_4 of [4-[1-(Benzenesulfonamido)alkyl]phenyl]alkanoic Acid Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
In order to find new antiasthmatic agents with dual antagonistic activity against thromboxane A_2 (TXA_2) and leukotriene D_4 (LTD_4) receptors, synthesis and pharmacological evaluation of various [4-[1-(benzenesulfonamido)-alkyl]phenyl]alkanoic acid derivatives were undertaken. TXA_2 and LTD_4 antagonistic activities in vitro were evaluated by measuring the inhibitory effects on U-46619-induced contraction of guinea-pig trachea and LTD_4-induced contraction of guinea-pig ileum and trachea. Several compounds showed satisfactory dual antagonistic activities, and their effect (after oral administration) on LTD_4-induced bronchoconstriction in guinea-pig in vivo was examined. The results demonstrated that both 4-[4-[1-(4-chlorobenzenesulfonamido)hexyl]phenyl]butyric acid (12e) and 4-[4-[1-(4-chlorobenzenesulfonamido)-5-methylhexyl]phenyl]butyric acid (12m) possessed good anti-LTD_4 activities. Compounds 12e and 12m were then evaluated for other related pharmacological effects involving the arachidonic acid cascade. These compounds appear to be hybrid eicosanoids antagonists having antagonistic activity against contraction of guinea-pig trachea induced by prostaglandin D_2 (PGD_2) and PGF_<2α>, as well as TXA_2 and LTD_4 antagonistic activities.
- 社団法人日本薬学会の論文
- 1997-05-15
著者
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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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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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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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ONOGI Yasuyo
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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TAKESHITA Makoto
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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TAKAHASHI Hiromi
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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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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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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Onogi Yasuyo
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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Ohashi Tetsuo
Research And Development Division Hokuriku Seiyaku Co. Ltd
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Takeshita M
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Sakurai S
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Takahashi Hiromi
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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