Sircar I, Duell B L, Bristol J A, Weishaar R E, Evans D B
J Med Chem. 1987 Jun;30(6):1023-9. doi: 10.1021/jm00389a011.
Several 1,2-dihydro-5-(substituted phenyl)-2(1H)-pyridinones were synthesized and evaluated for inotropic activity. 1,2-Dihydro-5-[4-(1H-imidazol-1-yl)phenyl]-6-methyl-2-oxo-3- pyridinecarbonitrile (5a) and the corresponding unsubstituted analogue 14a were the most potent positive inotropic agents in this series. Although the 4,6-dimethyl analogue 6a retained most of the activity of 5a, the 4-methyl analogue 8a was substantially less potent. The synthesis and structure-activity relationships are discussed.
合成了几种1,2 - 二氢 - 5 -（取代苯基）-2(1H)-吡啶酮，并对其变力活性进行了评估。1,2 - 二氢 - 5 - [4 -（1H - 咪唑 - 1 - 基）苯基]-6 - 甲基 - 2 - 氧代 - 3 - 吡啶甲腈（5a）和相应的未取代类似物14a是该系列中最有效的正性肌力药物。尽管4,6 - 二甲基类似物6a保留了5a的大部分活性，但4 - 甲基类似物8a的效力明显较低。讨论了合成方法和构效关系。
