title: Avermectins and flea control: structure-activity relationships and the selection of selamectin for development as an endectocide for companion animals.
abstract: 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.
authors.affiliation: Pfizer Central Research, Sandwich, Kent, UK. bernard_banks@sandwich.pfizer.com
authors.forename: B J
authors.initials: BJ
authors.lastname: Banks
authors.forename: B F
authors.initials: BF
authors.lastname: Bishop
authors.forename: N A
authors.initials: NA
authors.lastname: Evans
authors.forename: S P
authors.initials: SP
authors.lastname: Gibson
authors.forename: A C
authors.initials: AC
authors.lastname: Goudie
authors.forename: K A
authors.initials: KA
authors.lastname: Gration
authors.forename: M S
authors.initials: MS
authors.lastname: Pacey
authors.forename: D A
authors.initials: DA
authors.lastname: Perry
authors.forename: M J
authors.initials: MJ
authors.lastname: Witty
mesh_terms: D000818:Animals; D002415:Cats; D004285:Dogs; D005260:Female; D007306:Insecticides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D007559:Ivermectin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D015394:Molecular Structure; D005423:Siphonaptera; D021241:Spectrometry, Mass, Electrospray Ionization; D013329:Structure-Activity Relationship
chemical_list: D007306:Insecticides; D007559:Ivermectin; C019264:avermectin; C414354:selamectin