Structure-Activity Relationship of Anthelmintic Cyclooctadepsipeptides

被引：11

作者：

Ohyama, Makoto ^{[1
,2
]}

Okada, Yumiko ^{[3
]}

Takahashi, Masaaki ^{[3
]}

Sakanaka, Osamu ^{[3
]}

Matsumoto, Maki ^{[3
]}

Atsumi, Kunio ^{[1
,2
]}

机构：

[1] Tokyo Inst Technol, Interdisciplinary Grad Sch Sci & Engn, Dept Elect Chem, Midori Ku, Yokohama, Kanagawa 2268503, Japan

[2] Meiji Seika Kaisha Ltd, Pharmaceut Res Ctr, Kohoku Ku, Kanagawa 2228567, Japan

[3] Meiji Seika Kaisha Ltd, Chem Mfg & Control Res Labs, Kanagawa 2500852, Japan

来源：

BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY | 2011年 / 75卷 / 07期

关键词：

PF1022A; anthelmintic; structure-activity relationship; depsipeptide; CYCLODEPSIPEPTIDE; PF1022A; ANALOGS;

D O I：

10.1271/bbb.110129

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The relationship between cyclooctadepsipeptides and their anthelmintic efficacy was examined by converting the natural products, PF1022A, PF1022E and PF1022H. Some analogues substituted at the para position of the phenyllactate moiety showed higher or equivalent activity against the parasitic nematode, Ascaridia galli in chicken when compared with the parent compounds. It is suggested that lipophilicity and the polar surface area, in addition to structural requirements of the derivatives, influenced the anthelmintic efficacy in vivo.

引用

页码：1354 / 1363

页数：10

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