Avermectins and flea control: structure-activity relationships and the selection of selamectin for development as an endectocide for companion animals.
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.
Banks
B J
BJ
Pfizer Central Research, Sandwich, Kent, UK. bernard_banks@sandwich.pfizer.com
Bishop
B F
BF
Evans
N A
NA
Gibson
S P
SP
Goudie
A C
AC
Gration
K A
KA
Pacey
M S
MS
Perry
D A
DA
Witty
M J
MJ
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
D007306:Insecticides; D007559:Ivermectin; C019264:avermectin; C414354:selamectin