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

Autor: Banks BJ; Pfizer Central Research, Sandwich, Kent, UK. bernard_banks@sandwich.pfizer.com, Bishop BF, Evans NA, Gibson SP, Goudie AC, Gration KA, Pacey MS, Perry DA, Witty MJ
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2000 Aug; Vol. 8 (8), pp. 2017-25.
DOI: 10.1016/s0968-0896(00)00120-6
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: MEDLINE