Synthesis and paralytic activities of squaryl amino acid-containing polyamine toxins

被引：0

作者：

T. Shinada

Y. Nakagawa

K. Hayashi

G. Corzo

T. Nakajima

Y. Ohfune

机构：

[1] Graduate School of Science,

[2] Osaka City University,undefined

[3] Sugimoto,undefined

[4] Osaka,undefined

[5] Japan,undefined

[6] Suntory Institute for Bioorganic Research,undefined

[7] Shimamoto-cho,undefined

[8] Mishima-gun,undefined

[9] Osaka,undefined

[10] Japan,undefined

来源：

Amino Acids | 2003年 / 24卷

关键词：

Keywords: Philanthotoxin; Nephilatoxin-8; Polyamine toxins; Paralytic activity -Glutamate receptors; Squaric acid; Squaryl amino acid; 4-Hydroxycyclobuten-1-one; 2; 3-dioxocyclobutene; N-Acyl squaryl amino acid; Squaryl amino acid-containing polyamine toxins; Insecticidal activity;

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学科分类号：

摘要：

Eight analogs 4a-7a and 4b-7b of philanthotoxin (PhTX) from wasp venom and nephilatoxin-8 (NPTX-8) from spider venom whose tyrosine or asparagine linker is replaced by squaryl (sq) amino acid or 4-amino squaryl (4-asq) amino acid have been synthesized in an efficient manner via coupling of N-acyl squaryl amino acid intermediate 19 or 26 with the corresponding polyamine part. Preliminary bioassay using crickets revealed that the analogs substituted by glutamate-type squaryl amino acid-containing NPTX 7a and 7b showed more potent paralytic activities than that of NPTX-8.

引用

页码：293 / 301

页数：8