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

Autor: Banks, B.J., Bishop, B.F., Evans, N.A., Gibson, S.P., Goudie, A.C., Gration, K.A.F., Pacey, M.S., Perry, D.A., Witty, M.J.
Zdroj: Bioorganic & Medicinal Chemistry; August 2000, Vol. 8 Issue: 8 p2017-2025, 9p
Abstrakt: 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.
Databáze: Supplemental Index