A Novel Dual Antagonist of Thromboxane A_2 and Leukotriene D_4 Receptors : Synthesis and Structure-Activity Relationships of Chloroquinolylvinyl Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
To discover an orally active thromboxane A_2 (TXA_2) and leukotriene D_4 (LTD_4) dual antagonist, we designed and synthesized chloroquinolylvinyl derivatives based on the structures of the TXA_2 antagonist daltroban and the LTD_4 antagonist montelukast. Among these derivatives, 4-{[(2-(4-chlorophenylsulfonylamino)-1-{3-[(E)-2-(7-chloro-2-quinolyl)vinyl]phenyl}ethyl)thio]methyl}benzoic acid (18d) showed potent inhibitory activity against U46619-induced aggregation of guinea pig platelets and LTD_4-induced contraction in the guinea pig ileum, with IC_<50> values of 340nm and 0.40nm, respectively. Oral administration of 18d also inhibited both the LTD_4-induced acceleration of plasma leakage to skin in guinea pig and the U46619-induced increase in airway resistance in guinea pig with ED_<50> values of 0.47mg/kg and 3.3mg/kg, respectively.
- 公益社団法人日本薬学会の論文
- 2006-05-01
著者
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山本 修
Department Of Applied Chemistry Kanagawa Institute Of Technology
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Yamamoto O
広島国際大学 保健医療
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Takeuchi M
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Takeuchi Makoto
Chemistry Research Laboratories Astellas Pharmaceutical Inc.
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Takeuchi M
Chemistry Research Laboratories Astellas Pharmaceutical Inc.
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Yamamoto Osamu
Department Of Clinical Radiology Faculty Of Health Science Hiroshima International University
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Okamoto Y
Chemistry Research Laboratories Astellas Pharmaceutical Inc.
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Yokota Masaki
Chemistry Research Laboratories Astellas Pharmaceutical Inc.
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OKAMOTO Yoshinori
Chemistry Research Laboratories, Astellas Pharmaceutical Inc.
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KAWAZOE Soichiro
Process Chemistry Laboratories, Astellas Pharmaceutical Inc.
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KUBOTA Hirokazu
Chemistry Research Laboratories, Astellas Pharmaceutical Inc.
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ARAKIDA Yasuhito
Planning & Administration Dept., Astellas Pharmaceutical Inc.
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Kawazoe Soichiro
Process Chemistry Laboratories Astellas Pharmaceutical Inc.
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Arakida Yasuhito
Planning & Administration Dept. Astellas Pharmaceutical Inc.
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Kubota H
Chemistry Research Laboratories Astellas Pharmaceutical Inc.
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Kurihara H
Chemistry Research Laboratories Astellas Pharmaceutical Inc.
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Ohyama Yoshihiko
Facul. Sci. Hiroshima Univ.
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