Ogawa K, Miyoshi K
Taiho Pharmaceutical Company, Ltd., Tokushima Research Laboratory, Japan.
J Pharm Sci. 1992 Jun;81(6):581-5. doi: 10.1002/jps.2600810624.
Two series of 3,6-dimethyl-1-phenyl-1H-pyrazolo[4,3-c] pyridine-4-ones (5-9) and 3,6-dimethyl-1-phenyl-1H-pyrazolo[4,3-c] pyridine-4-thiones (11-13) were prepared from dehydroacetic acid as starting material and evaluated for positive inotropic activity in vitro. Moreover, the activity of the synthesized compounds was compared with that of mirlinone as a reference. Among these compounds, the positive inotropic activity of 8a, 11a, and 12 were approximately 1.24, 1.77, and 1.11 times more potent, respectively, than that of mirlinone.
以脱氢乙酸为起始原料制备了两个系列的3,6 - 二甲基 - 1 - 苯基 - 1H - 吡唑并[4,3 - c]吡啶 - 4 - 酮（5 - 9）和3,6 - 二甲基 - 1 - 苯基 - 1H - 吡唑并[4,3 - c]吡啶 - 4 - 硫酮（11 - 13），并对其体外正性肌力活性进行了评估。此外，将合成化合物的活性与米力农作为参比进行了比较。在这些化合物中，8a、11a和12的正性肌力活性分别比米力农强约1.24倍、1.77倍和1.11倍。
