文章基本信息

标题：Biological Activities of 1, 1, 6-Trisubstituted Indanes : Beyond Magainin 2
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作者：Naganori NUMAO ; Yukiko HIROTA ; Akiyo IWAHORI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1999
卷号：22
期号：1
页码：73-76
DOI：10.1248/bpb.22.73
出版社：The Pharmaceutical Society of Japan
摘要：MSI-78 is a peptide analog of naturally occurring magainin 2 isolated from the skin of Xenopus laevis. The peptide is known to have one of the strongest antibacterial activities in magainin 2 analogs against methicillin-resistant Staphylococcus aureus (MRSA). To find novel compounds superior to MSI-78, we have further designed, synthesizing 1, 1-di(4-aminobutyl)-6-benzylindane (PM4) and 1, 1-dibenzyl-6-(4-aminobutyl) indane (PM5), and tested their inhibitory ability of the growth of S. aureus. In an in vitro assay, PM4 showed the same antibacterial activity against the bacterium as MSI-78, and non-hemolytic activity against human red blood cells (RBCs) at the MIC (minimum inhibitory concentration )value, in contrast to the latter. On the other hand, PM 5 showed stronger antibacterial activity than MSI-78, but being still accompanied with hemolysis at the MIC value. Otherwise, stronger decarboxylase activity for oxaloacetate was observed in PM5, rather than magainin 2 analogs or Oxaldie 1 as a control peptide, but not in PM4.
关键词：magainin 2 analog;antibacterial activity;decarboxylase activity;peptidomimetic;indane derivative;S. aureus