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D A Ostlind

Publications and source records attributed to D A Ostlind.

34 records · Page 2Linked to original sources

Substituted imidazo[2,3-alpha]pyridine-2-carbamate anthelmintics.

Anthelmintic efficacies of a series of 6-substituted methyl imidazo[1,2-alpha]pyridine-2-carbamates were compared to similarly substituted benzimidazole-2-carbamates. With only one exception, methyl 6-benzoylimidazo[1,2-alpha]pyridine-2-carbamate, both classes of compounds exhibited similar activity vs. Nematospiroides dubius in mice. Preliminary screening indicated methyl 6-(1,2,2-trichloroethenyl)imidazo[1,2-alpha]pyridine-2-carbamate to be the most potent derivative in the series. However, evaluation in sheep indicated that its anthelmintic spectrum was inferior to methyl 6-(phenylsulfinyl)imidazo[1,2-alpha]pyridine-2-carbamate.

Animals↗

Ivermectin, a new broad-spectrum antiparasitic agent.

22,23-Dihydroavermectin B1, ivermectin, derived from avermectin B1 by selective hydrogenation using Wilkinson's homogenous catalyst [Ph3P)3RhCl], was shown to be a highly effective drug for the treatment of a wide variety of metazoan parasitic diseases in animals.

Animals↗

Avermectins, new family of potent anthelmintic agents: efficacy of the B1a component.

When given to sheep as a single oral dose at 0.1 mg/kg, the B(1a) component of the avermectins caused a reduction of >95% in the numbers of Haemonchus contortus, Ostertagia circumcincta (including inhibited L(4) larvae), Trichostrongylus axei, Trichostrongylus colubriformis, Cooperia oncophora, and Oesophagostomum columbianum. When given to cattle as a single oral dose at 0.1 mg/kg, avermectin B(1a) was >95% effective in reducing the numbers of Haemonchus placei, Ostertagia ostertagi (including inhibited L(4) larvae), T. axei, T. colubriformis, C. oncophora, Cooperia punctata, Oesophagostomum radiatum, and Dictyocaulus viviparus. Avermectin B(1a) was similarly effective, with the exception of a detectable loss in activity against adult C. oncophora, when administered to cattle as a parenteral injection. Some of these ruminant parasites were fully susceptible to dosages of avermectin B(1a) at 0.025 mg/kg, e.g., D. viviparus, O. radiatum, O. ostertagi, and H. contortus. Avermectin B(1a) removed 83 to 100% of Ancylostoma caninum from dogs given a single oral dose of 0.003 to 0.005 mg/kg. The poultry nematodes Capillaria obsignata and immature Ascaridia galli were effectively removed by avermectin B(1a) at 0.05 and 0.1 mg/kg, respectively, but 0.1 mg/kg was not effective for Heterakis gallinarum. Thus, the avermectins would appear to have unprecedented potency and spectrum of biological activity.

Administration, Oral↗

Methyl 6-(phenylsulfinyl)imidazo[1,2-a]pyridine-2-carbamate, a potent, new anthelmintic.

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.

Animals↗

4-amino-6-(trichloroethenyl)-1,3-benzenedisulfonamide, a new, potent fasciolicide.

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.

Animals↗