| 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. |
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