Since the discovery of orally-bioavailable isoxazolines in the mid-2000's, multiple animal health companies have engaged in active discovery efforts to develop a new oral product with broad spectrum flea and tick control for at least one month in a single dose. The Zoetis research team has been successful in identifying a proprietary spiro-azetidine isoxazoline (Sarolaner) which meets the required <i>in vitro</i> and <i>in vivo</i> profiles for once-a-month dosing. The design, synthesis, and biological activity of spiro-azetidine isoxazoline analogs, ultimately leading to the selection of Sarolaner, will be presented.

Spiro-azetidine isoxazolines: The discovery of a new class of oral flea and tick parasiticides in canines

256th National Meeting (2018)

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