Synthetic Studies on Condensed-Azole Derivatives. I. Synthesis and Anti-asthmatic Activities of ω-Substituted Alkylthioimidazo[1,2-b]pyridazines

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概要

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• A series of novel ω-substituted alkylthioimidazo[1,2-b]pyridazines was designed and synthesized in an effort to find a novel anti-asthmatic agent. The anti-asthmatic activity of these compounds was evaluated ont he basis of their ability to inhibit thromboxane A_2 synthetase and platelet activating factor (PAF)-induced bronchoconstriction in guinea pigs. None of these compounds significantly inhibited thromboxane A_2 synthetase, though, sulfonamide derivatives potently inhibited PAF-induced bronchoconstriction. Among them, 3-(imidazo[1,2-b]pyridazin-6-yl)thiopropanesulfonamide (5) showed the most potent inhibitory effect. The anti-asthmatic effects of compound 5 in experimental models were superior to those of theophylline.

• 社団法人日本薬学会の論文
• 1995-09-15

著者

• 桑原 雅明

  Pharmaceutical Research Division, Pharmaceutical Research Laboratories III Takeda Chemical Industrie

• 三宅 昭夫

  Pharmaceutical Research Division, Pharmaceutical Research Laboratories III Takeda Chemical Industrie

• 川野 泰彦

  Pharmaceutical Research Division, Pharmaceutical Research Laboratories III, Takeda Chemical Industir

• 蘆田 康子

  Pharmaceutical Research Laboratories II, Takeda Chemical Industries, Ltd.,

• 蘆田 康子

  武田薬品・創薬研究本部

• 川野 泰彦

  Pharmaceutical Research Division Pharmaceutical Research Laboratories Iii Takeda Chemical Industries

• 河合 龍彦

  Pharmaceutical Research Division, Pharmaceutical Research Laboratories III, Takeda Chemical Industri

• 三宅 昭夫

  武田薬品・創薬研究本部

• 河合 龍彦

  Pharmaceutical Research Division Pharmaceutical Research Laboratories Iii Takeda Chemical Industries

• 桑原 雅明

  Pharmaceutical Research Division Pharmaceutical Research Laboratories Iii Takeda Chemical Industries

• Miyake Akio

  Pharmaceutical Research Division Pharmaceutical Research Laboratories Ii Research Promotion Takeda C

• Kuwahara Masaaki

  Pharmaceutical Research Division Pharmaceutical Research Laboratories Ii Research Promotion Takeda C

• 蘆田 康子

  Pharmaceutical Research Laboratories Ii Takeda Chemical Industries Ltd.

• Kawano Y

  Otsuka Pharmaceutical Co. Ltd. Tokushima Jpn

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