Avermectins and flea control: Structure-activity relationships and the selection of selamectin for development as an endectocide for companion animals

被引：29

作者：

Banks, BJ ^{[1
]}

Bishop, BF ^{[1
]}

Evans, NA ^{[1
]}

Gibson, SP ^{[1
]}

Goudie, AC ^{[1
]}

Gration, KAF ^{[1
]}

Pacey, MS ^{[1
]}

Perry, DA ^{[1
]}

Witty, MJ ^{[1
]}

机构：

[1] Pfizer Ltd, Cent Res, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2000年 / 8卷 / 08期

关键词：

D O I：

10.1016/S0968-0896(00)00120-6

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：

Evaluation of a wide range of avermectin derivatives for flea activity in an in vitro feeding screen using the cat flea, Ctenocephalides felis, revealed a narrow structure-activity relationship (SAR) with activity surprisingly associated with monosaccharides and especially their C-5-oximes. We discovered commercially exploitable flea activity in a single compound, selamectin 33, which also possessed the necessary antiparasitic spectrum and margin of safety for development as a broad-spectrum companion animal endectocide. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2017 / 2025

页数：9

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