Design, Synthesis, and Monoamine Oxidase Inhibitory Activity of (+)-Cinchonaminone and Its Simplified Derivatives

Yuta Sato, Naoko Oyobe, Takao Ogawa, Sayo Suzuki, Hiroshi Aoyama, Tomonori Nakamura, Hiromichi Fujioka, Satoshi Shuto, Mitsuhiro Arisawa

研究成果: Article査読

抄録

The absolute structure of an indole alkaloid (+)-cinchonaminone by total synthesis of both (+)-cinchonaminone and its enantiomer was determined. The main focus of the study was the enantioselective synthesis of both enantiomers of a chiral cis-3,4-disubstituted piperidine. We also evaluated monoamine oxidase (MAO) inhibitory activities of these enantiomers. Furthermore, its structurally simplified derivatives were synthesized that did not have any chiral center. Two of these derivatives showed stronger MAO inhibitory activities than that of (+)-cinchonaminone.

本文言語English
ページ(範囲)1464-1469
ページ数6
ジャーナルACS Medicinal Chemistry Letters
12
9
DOI
出版ステータスPublished - 2021 9 9

ASJC Scopus subject areas

  • 生化学
  • 創薬
  • 有機化学

フィンガープリント

「Design, Synthesis, and Monoamine Oxidase Inhibitory Activity of (+)-Cinchonaminone and Its Simplified Derivatives」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル