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4.
J Med Chem ; 21(2): 235-7, 1978 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-621722

RESUMEN

A series of methyl imidazo-[11,2-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 and 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.


Asunto(s)
Antihelmínticos/síntesis química , Carbamatos/síntesis química , Piridinas/síntesis química , Animales , Antihelmínticos/uso terapéutico , Carbamatos/farmacología , Carbamatos/uso terapéutico , Bovinos , Perros , Ratones , Infecciones por Nematodos/tratamiento farmacológico , Piridinas/farmacología , Piridinas/uso terapéutico , Ovinos , Porcinos
5.
J Med Chem ; 20(9): 1225-7, 1977 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-926125

RESUMEN

The synthesis and fasciolicidal activity of 4-amino-6-(trichloroethenyl)-1,3-benzenedisulfonamide are reported. A single dose of 15 mg/kg was effective in removing over 90% of immature Fasciola hepatica from sheep (6 weeks after infection) and calves (8 weeks after infection). A 2.5 mg/kg dose removed over 90% of mature (16 weeks old) liver fluke from sheep. Single oral doses up to 400 mg/kg were tolerated by sheep without gross toxic symptoms.


Asunto(s)
Antihelmínticos/uso terapéutico , Fascioliasis/tratamiento farmacológico , Sulfonamidas/uso terapéutico , Animales , Antihelmínticos/síntesis química , Antihelmínticos/toxicidad , Bovinos , Fasciola hepatica , Ovinos , Sulfanilamidas , Sulfonamidas/síntesis química , Sulfonamidas/toxicidad , Tricloroetileno/análogos & derivados , Tricloroetileno/síntesis química , Tricloroetileno/uso terapéutico
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