Isoxazole anthelmintics

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Abstract
A series of 3-halo-5-phenyl- and 3-phenyl-5-haloisoxazoles demonstrated anthelmintic activity at doses ranging from 16-500 mg/kg orally against the rat roundworm, Nippostrongylus braziliensis. In the 5-phenyl series a halogen at the 3 position of the isoxazole ring was required for activity. In the 3-phenyl series activity was maintained after replacement of the 5-halogen with certain alkoxyl, thioalkoxyl or amino groups. The 3-phenyl and 5-phenyl series apparently are not acting biologically at a common receptor site. Synthetic methods and structure-activity relationships are discussed.

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