縮合Pyridazine誘導体の合成研究(第3報)縮合Triazolopyridazine誘導体の合成とBenzodiazepine受容体親和性

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概要

• 論文の詳細を見る

• A series of 6H-(1) benzothiopyrano [3,4-e] [1,2,4] triazolo [4,3-b] pyridazines and 6,7-dihydro-(1) benzothiepino [4,5-e] [1,2,4] triazolo [4,3-b] pyridazines were prepared and tested for their ability to displace [^3H] diazepam from rat brain membranes. An approximately planar shape of these molecules was essential for high affinity to the benzodiazepine receptor. Among them, 11-aryl compounds in the latter series were found to have high affinity to the benzodiazepine receptor. 11-Phenyl- and 11-thienyl-6,7-dihydro-(1) benzothiepino [4,5-e] [1,2,4] triazolo [4,3-b] pyridazine (3b-5 and 3b-11 respectively) showed the potent affinity comparable to that of diazepam. The structure-activity relationships are also discussed.

• 公益社団法人日本薬学会の論文
• 1990-12-25

著者

• 田中 寛

  三菱ウェルファーマ株式会社・研究本部

• 中尾 達

  Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.,

• 森本 保人

  Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.,

• 田原 哲治

  Research Laboratories Yoshitomi Pharmaceutical Industries Ltd.

• 中尾 達

  Research Laboratories Yoshitomi Pharmaceutical Industries Ltd.

• 竹原 修治

  Research Laboratories Yoshitomi Pharmaceutical Industries Ltd.

• 田中 寛

  吉富製薬株式会社中央研究所

• 森本 保人

  吉富製薬株式会社中央研究所

• 竹原 修造

  吉富製薬株式会社中央研究所

• 出水 賢一

  吉富製薬株式会社中央研究所

• 田原 哲冶

  吉富製薬株式会社中央研究所

• 出水 賢一

  吉富製薬(株)中央研究所

• 森本 保人

  Research Laboratories Yoshitomi Pharmaceutical Industries Ltd.

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• 縮合Pyridazine誘導体の合成研究(第3報)縮合Triazolopyridazine誘導体の合成とBenzodiazepine受容体親和性
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