Synthesis and Muscarinic Activity of Novel Aniline Derivatives with a 1-Azabicyclo[3.3.0]octane Moiety

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概要

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• In order to develop drugs effective against Alzheimer's disease, we synthesized a series of aniline derivatives having a characteristic cyclic amine, 1-azabicyclo[3.3.0]octane ring, and evaluated their binding affinity for the central muscarinic cholinergic receptor.Among these compounds which showed high affinity to the M_1 receptor, N-[2-(1-Azabicyclo[3.3.0]octan-5-yl)ethyl]-2-nitroaniline (9f fumarate, SK-946) showed the highest affinity. The ability of this compound to improve cognitive function was assessed using the passive avoidance test in scopolamine-induced dementia mice.Some anilines with a 1-azabicyclo[3.3.1]nonane ring were also synthesized by the ring expansion of the 1-azabicyclo[3.3.0]octane ring, and showed a high affinity for the central muscarinic cholinergic receptor.

• 公益社団法人日本薬学会の論文
• 1999-01-15

著者

• KATAOKA Tadashi

  Gifu Pharmaceutical University

• SUZUKI Tomoo

  Drug Discovery Research Department, Sanwa Kagaku Kenkyusho Co., Ltd.,

• MAEDA Kouji

  Drug Discovery Research Department, Sanwa Kagaku Kenkyusho Co., Ltd.,

• UESAKA Hiroshi

  Drug Development Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.,

• OKA Mitsuru

  Drug Discovery Research Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.,

• FURUSAWA Kenichi

  Drug Development Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.,

• Furusawa K

  Pharmaceutical Laboratory Sanwa Kagaku Kenkyusho Co. Ltd.

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