
Journal of Medicinal Chemistry p. 235 - 237 (1978)
Update date:2022-08-03
Topics: Chemical Synthesis In vitro Testing In Vivo Testing Experimental terms Anthelmintic
Bochis
Dybas
Eskola
Kulsa
Linn
Lusi
Meitzner
Milkowski
Mrozik
Olen
Peterson
Tolman
Wagner
Waksmunski
Egerton
Ostlind
A series of methyl imidazo[1,2-a]pyridine-2-carbamates was synthesized for anthelmintic testing. The preparation of this class of compounds was simplified by utilization of a novel one-step condensation of the appropriately substituted 2-aminopyridine with methyl chloroacetylcarbamate. The most potent compound, methyl 6-(phenylsulfinyl) imidazo[1,2-a] pyridine-2-carbamate, was orally effective against a broad range of helminths in sheep and cattle, at a dosage of 2.5 mg/kg. Limited trials in swine and dogs demonstrated anthelmintic activity at higher dosages. Limited observations in sheep and cattle indicated that, in both species, a single oral dose of 200 mg/kg was well tolerated.
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