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
| Autor: | Kinichi Imai, Toshimi Matsuno, T. Seo, Mitsuhiko Mano |
|---|---|
| Rok vydání: | 1981 |
| Předmět: |
Orotic acid
Pyrazine Oxide chemistry.chemical_element General Chemistry General Medicine Peroxide Medicinal chemistry Turn (biochemistry) chemistry.chemical_compound Hydrolysis Nickel chemistry Pyrazines Drug Discovery medicine Organic chemistry Animals Coccidiostats Amine gas treating Chickens medicine.drug |
| Zdroj: | Chemicalpharmaceutical bulletin. 29(1) |
| ISSN: | 0009-2363 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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