Synthesis and pharmacological properties of N,N-dialkyl(dialkenyl)amides of 7-methyl-3-phenyl-1-[2-hydroxy-3-(4-phenyl-1-piperazinyl)propyl]-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-5-carboxylic acid
| Autor: | Aleksandra Sabiniarz, Malgorzata Kardasz, Dorota Maciag, Helena Sladowska, Barbara Filipek |
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| Rok vydání: | 2003 |
| Předmět: |
Male
Pyrimidine Pyridones medicine.drug_class Stereochemistry Carboxylic acid Carboxylic Acids Pharmaceutical Science Carboxamide Motor Activity Medicinal chemistry Chemical synthesis Mice chemistry.chemical_compound Drug Discovery medicine Animals Rats Wistar Pain Measurement chemistry.chemical_classification Bicyclic molecule Biological activity General Medicine Rats Pyrimidines chemistry Mechanism of action Barbiturate medicine.symptom |
| Zdroj: | Il Farmaco. 58:25-32 |
| ISSN: | 0014-827X |
| Popis: | Synthesis of N , N -dialkyl(dialkenyl)amides of 7-methyl-3-phenyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3- d ]pyrimidine-5-carboxylic acid ( 5 – 9 ) and their 1-[2-hydroxy-3-(4-phenyl-1-piperazinyl)propyl] derivatives ( 10 – 14 ) is described. Compounds 10 – 14 were tested for analgesic and sedative activities as well as for μ-opioid receptors binding affinities. All the amides, being the object of investigation, displayed an interesting analgesic action, which in case of the compounds 10 – 12 and 14 was superior to that of acetylsalicylic acid in two different tests. Furthermore all the amides ( 10 – 14 ) significantly suppressed the spontaneous locomotor activity, prolonged barbiturate sleep in mice and showed a weak affinity to μ-opioid receptors. |
| Databáze: | OpenAIRE |
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