Gómez-Parra V, Gómez M C, Sánchez F, Stefani V
Instituto de Química, Universidad Federal do Rio Grande do Sul, BR-91500 Porto Alegre, Brazil.
Arch Pharm (Weinheim). 1992 Aug;325(8):483-90. doi: 10.1002/ardp.19923250807.
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.
为开发新型强心剂，已从甲基喹啉、2-芳基乙酸或3-芳基乙酮出发，通过直接氨甲基化，随后在经典碱性介质或相转移催化条件下与丙二酰胺和氰基乙酰胺进行缩合环化反应，制备了一系列与氨力农相关的5-芳基-3,4-二氢吡啶-2(1H)-酮，产率良好至优异。初步药理试验表明，这些化合物，尤其是5h和5i，具有显著的强心作用，并对从猫心脏分离出的磷酸二酯酶III/磷酸二酯酶I有选择性抑制作用。
