New Cardiotonic Agents Related to Amrinone: Synthesis of 1,2-Dihydro-5-arylpyridin-2-ones
| Autor: | Valter Stefani, Félix Sánchez, M. Del Carmen Gomez, Vicente Gómez-Parra |
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| Rok vydání: | 1992 |
| Předmět: |
Cardiotonic Agents
biology Pyridones Stereochemistry Guinea Pigs Pharmaceutical Science Biological activity In Vitro Techniques Selective inhibition Amrinone Myocardial Contraction Combinatorial chemistry Phosphodiesterase I chemistry.chemical_compound chemistry Enzyme inhibitor Drug Discovery Cats medicine Lactam biology.protein Animals medicine.drug |
| Zdroj: | Scopus-Elsevier |
| ISSN: | 1521-4184 0365-6233 |
| DOI: | 10.1002/ardp.19923250807 |
| Popis: | For development of new cardiotonic agents a series of 5-aryl-3,4-dihydropyridin-2(1H)-ones, related to amrinone have been prepared from methylquinolines, 2-arylacetic acid or 3-arylethanones by direct aminomethylenation and subsequent condensation-cyclization with malonamide and cyanacetamide in classic basic media or phase-transfer catalysis, in good to excellent yields. Preliminary pharmacological assays have shown that these compounds, especially 5h and 5i, have a remarkable cardiotonic effect and present a selective inhibition of PDE-III/PDE-I isolated from cat heart. |
| Databáze: | OpenAIRE |
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