Imidazo[1,2-α]pyridines. III. Synthesis and Bradycardic Activity of New 5-Imidazo[1,2-a]pyridin-6-ylpyridine Derivatives

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概要

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• Structural modification of the cardiotonic agent, loprinone (E-1020,1), suggested by data that it has a less positive chronotropic effect than milrinone (15), led us to find novel bradycardic agents that were structurally different from homoveratry amine derivatives. Alkyl-oxy, -thio, and -amino derivatives at the 2-position of the pyridine ring of 1 produced bradycardic activity without a significant effect on blood pressure and myocardial contractility. Aryloxy analogues also decreased heart rate, and members with an electron-withdrawing group at the ortho position of the phenyl ring showed higher activity. Replacement of the imidazo[1,2-a]pyridine with pyridine resulted in diminished activity. The mechanism of bradycardic activity of these compounds seems to be direct action on the sinus node.

• 公益社団法人日本薬学会の論文
• 1992-06-25

著者

• 川村 高紀

  Eisai Research Institute

• 川村 高紀

  Eisai Tsukuba Research Laboratories

• 山中 基資

  Eisai Tsukuba Research Laboratories

• 須田 眞次

  Eisai Tsukuba Research Laboratories

• 樺沢 靖弘

  Eisai Tsukuba Research Laboratories

• 小川 利明

  Eisai Tsukuba Research Laboratories

• 澤田 光平

  Eisai Tsukuba Research Laboratories

• 大原 秀人

  Eisai Tsukuba Research Laboratories

• 山中 基資

  Eisai Co. Ltd. Tsukuba Research Laboratories

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