The Site of Action of a Broad-Spectrum Aryltriazine Anticoccidial, CP-25,415

Chappel, Larry R.; Howes, Harold L.; Lynch, John E.

doi:10.2307/3278354

Cited by 26 publications

(7 citation statements)

References 5 publications

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“…Addition of 400 mL of water gave a solid which was collected by filtration. Recrystallization from EtOH-H20 gave 26.4 g of 2-[2-(3-acetamidophenyl)ethyl]-5-chlorobenzoic acid (35): mp 122-124 °C; NMR (Me2SO-d6) 2.12 (s, 3 H, CH3CO), 2.6-3.5 (m, 4 H, CH2CH2), 6.S-7.9 (m, 7 H, aryl H), 9.83 (s, 1 H, C02H). Anal.…”

Section: Methodsmentioning

confidence: 99%

Tricyclic aryl-substituted anticoccidial azauracils

Kluge¹,

Caroon²,

Unger³

et al. 1978

J. Med. Chem.

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Syntheses of tricyclic aryl-substituted 6-azauracils are described. These compounds showed anticoccidial activity when tested against Eimeria tenella and E. necatrix. Compound activity was correlated with the chemical shift of the azauracil ring proton. No correlation existed between activity and compound lipophilicity. One of the compounds, 2-(11-oxo-6,11-dihydrodibenzo[b,e]thiepin-3yl)-as-triazine-3,5(2H,4H)-dione (23), was tested extensively against E. tenella and E. brunetti both in vivo and in vitro. Compound 23 controlled mortality due to E. tenella at 62 ppm, and it afforded protection as measured by weight gain at 31 ppm. Compound 23 afforded little protection against E. brunetti. In vitro experiments with 23 showed that it exerted a coccidiostatic effect.

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Section: Methodsmentioning

confidence: 99%

Tricyclic aryl-substituted anticoccidial azauracils

Kluge¹,

Caroon²,

Unger³

et al. 1978

J. Med. Chem.

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“…Group sizes were three birds for E. tenella and five for the intestinal species. Lesions in the appropriate region of the intestine or ceca were scored at 6 days postinoculation (5 days for E. acervulina) as described by Chappel et al (1974), and weight gain over the test period was determined. The means of the semduramicin groups were compared to the salinomycin group by student's t test.…”

Section: In Vivo Screeningmentioning

confidence: 99%

“…In vivo screening was conducted as described previously (Chappel et al, 1974). Briefly, in-feed medication of White Leghorn chicks began at 10 days of age.…”

Section: In Vivo Screeningmentioning

confidence: 99%

Anticoccidial Efficacy of Semduramicin in Battery Studies with Laboratory Isolates of Coccidia

et al. 1992

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The anticoccidial activity of semduramicin against laboratory isolates of five species of poultry Eimeria was investigated. In laboratory scale battery trials, semduramicin at 20 to 30 ppm demonstrated broad-spectrum anticoccidial efficacy equivalent to salinomycin at 60 ppm. Also, semduramicin at 25 ppm was fed to uninfected cockerels in batteries for 21 days, and growth rate and feed efficiency were found to be equivalent to birds fed salinomycin at 60 ppm. Semduramicin was well tolerated when coadministered with tiamulin. Semduramicin demonstrated the same activity whether produced by semisynthesis or by direct fermentation.

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“…5 C: caled, 57.14; found, 56.65. N: caled, 18.17; found, 18.97. f C: caled, 59.50; found, 59.09. u C: caled, 48.71; found, 48.28 °Also sometimes called the minimum inhibitory concentration or MIC. Use levels may be higher in order to ensure adequate medication during periods of reduced feed intake and to prevent resistance development.…”

Section: Id >250mentioning

confidence: 99%

Anticoccidial derivatives of 6-azauracil. 1. Enhancement of activity by benzylation of nitrogen-1. Observations on the design of nucleotide analogs in chemotherapy

Mylari¹,

Miller²,

Howes³

et al. 1977

J. Med. Chem.

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Benzylation of 6-azauracil at N-1 (which corresponds to the point of attachment of the ribose phosphate unit in pyrimidine nucleotides) has been found to augment its anticoccidial activity fourfold. The high potency of 1-benzyl-6-azauracil is ascribed to a combination of intrinsic activity, efficient oral absorption, and a moderate rate of excretion. Metabolism experiments using 1-benzyl-6-azauracil labeled with 14C in the heterocycle and (separately) in the side chain showed that, in the drug accounted for, no cleavage had occurred. Additional activity increases were achieved by introducing small, electron-withdrawing substituents in the meta and/or para position(s) of the benzyl group. One of the most active derivaties, 1-(3-cyanobenzyl)-6-azauracil, is about 16 times as potent as 6-azauracil.

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The Site of Action of a Broad-Spectrum Aryltriazine Anticoccidial, CP-25,415

Cited by 26 publications

References 5 publications

Tricyclic aryl-substituted anticoccidial azauracils

Tricyclic aryl-substituted anticoccidial azauracils

Anticoccidial Efficacy of Semduramicin in Battery Studies with Laboratory Isolates of Coccidia

Anticoccidial derivatives of 6-azauracil. 1. Enhancement of activity by benzylation of nitrogen-1. Observations on the design of nucleotide analogs in chemotherapy

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