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文章基本信息

  • 标题:Development of Irreversible Inactivators of Spermine Oxidase and N 1-Acetylpolyamine Oxidase
  • 本地全文:下载
  • 作者:Shun-suke Moriya ; Toshiyuki Miura ; Koichi Takao
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2014
  • 卷号:37
  • 期号:3
  • 页码:475-480
  • DOI:10.1248/bpb.b13-00913
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:

    Three functional groups (2-propenyl, 2-propynyl, and 2,3-butadienyl) were introduced onto one of the terminal amino groups of spermidine. Of the six compounds synthesized, N -(3-aminopropyl)- N ′-2,3-butadienyl-1,4-butanediamine ( N 8-butadienyl Spd) and N -[3-(2,3-butadienylamino)propyl]-1,4-butanediamine ( N 1-butadienyl Spd) irreversibly inactivated human spermine oxidase (SMO) and N 1-acetylpolyamine oxidase (APAO). Interestingly, N 8-butadienyl Spd inactivated SMO far more potently than N , N ′-di-2,3-butadienyl-1,4-butanediamine (MDL 72527).

  • 关键词:spermine oxidase; N 1-acetylpolyamine oxidase; irreversible inhibitor; MDL 72527; polyamine catabolism
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