Anticoccidials. VI. An improved synthesis of 1,6-dihydro-6-oxo-2-pyrazinecarboxylic acid 4-oxide and some related derivatives and determination of anticoccidial activity.

doi:10.1248/CPB.29.88

Paper

Anticoccidials. VI. An improved synthesis of 1,6-dihydro-6-oxo-2-pyrazinecarboxylic acid 4-oxide and some related derivatives and determination of anticoccidial activity.

Published Jan 25, 1981 · K. Imai, M. Mano, T. Seo

Chemical & pharmaceutical bulletin

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7

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Abstract

1, 6-Dihydro-6-oxo-2-pyrazinecarboxylic acid 4-oxide (1) has been synthesized by two different methods. The first is a hydrolysis of methyl 6-chloro-2-pyrazinecarboxylate 4-oxide, which was in turn obtained from methyl 6-chloro-2-pyrazinecarboxylate by reaction with m-chloroperbenzoic acid. The second is an oxidation of 6-hydroxymethyl-2 (1H)-pyrazinone 4-oxide with nickel peroxide. Compound 1 was converted to amine salts, esters and amides. 6-Methoxy, 6-mercapto and 1-alkyl derivatives were also prepared. The compounds prepared were tested for anticoccidial activity in chickens against Eimeria tenella and marked activity was seen with compound 1 and amine salts of 1. The activity of 1 was counteracted by the simultaneous administration of an equal weight of orotic acid or adenine.

Study Snapshot

Compound 1,6-dihydro-6-oxo-2-pyrazinecarboxylic acid 4-oxide, and its amine salts, show marked anticoccidial activity in chickens against Eimeria tenella, with activity counteracted by orotic acid or adenine.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Anticoccidials. VI. An improved synthesis of 1,6-dihydro-6-oxo-2-pyrazinecarboxylic acid 4-oxide and some related derivatives and determination of anticoccidial activity.

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References

Citations

Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligands.

Diazabicyclo[3.3.0]octane-substituted pyridines and pyrazines show promising potential as potent 42 nicotinic acetylcholine receptor ligands with limited agonist activity.

Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.

Orally bioavailable 6-aryl-2-pyrazinecarboxamides effectively block the human Na(v)1.8 sodium channel, reducing neuropathic pain and reducing adverse events in a rodent model.

Eimeria tenella, E. necatrix, E. acervulina, and E. maxima: anticoccidial activity of 1,6-dihydro-6-oxo-2-pyrazinecarboxylic acid 4-oxide.

Carboxyemimycin effectively inhibits the development of Eimeria tenella in cockerels, without reducing weight gains.

Chapter 14. Antiparasitic Agents

This chapter highlights the pharmacokinetics, metabolism, and adverse reactions of antiparasitic agents, including 5-nitroimidazoles, congocidine derivatives, and A-33853, as well as their potential role in treating various protozoa and bacteria.