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  • 标题:Antibacterial Activity of Two Alkylamines Integrated an Indane Scaffold : Mimicry of a Complementary Unit on Magainin 2
  • 本地全文:下载
  • 作者:Naganori NUMAO ; Akiyo IWAHORI ; Yukiko HIROTA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1997
  • 卷号:20
  • 期号:7
  • 页码:800-804
  • DOI:10.1248/bpb.20.800
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Based on the antibacterial activity of 9-phenylnonylamine (pC9a) against Escherichia coli (ATCC29522) and Staphylococcus aureus (ATCC25923), we have further tested the inhibitory ability of the growth of the bacteria by (±)1-(4-aminobutyl)-6-benzylindane (PM2) and (±)1-benzyl-6-(4-aminobutyl) indane (PM3), that is, two kinds of 1, 6-disubstituted indanes. In an in vivo assay, they showed almost the same antibacterial activities against the bacteria as pC9a, as well as that of magainin 2 analogs (i.e., the peptides MSI-78 and 87-ISM), except in the case of 87-ISM against S. aureus. At the MIC (minimum inhibitory concentration) values, however, their killing rate of E.coli is actually quicker than pC9a. This indicates that an indane scaffold, used as a template to mimic a part of the α-helical structure of magainin 2, can accelerate the killing rate. At present, however, it is unknown wherther either the hydrophobicity or the α-helical structure, or both, of the indane scaffold is involved in accelerating the rate. Moreover, these two indanes also showed stronger antibacterial activity against two strains of Helicobacter pylori (ATCC43526, ATCC43579) than either pC9a or magainin 2 related peptides.
  • 关键词:magainin 2;complementary peptidomimetic;KF;indane scaffold;antibacterial activity;H. pylori
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