Synthesis and inotropic activity of pyrazolo[4,3-c]pyridine-4-ones and related compounds.
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.
Ogawa
K
K
Taiho Pharmaceutical Company, Ltd., Tokushima Research Laboratory, Japan.
Miyoshi
K
K
D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D009200:Myocardial Contraction / Q000187:drug effects; D010210:Papillary Muscles / Q000187:drug effects; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011728:Pyridones / Q000138:chemical synthesis* / Q000494:pharmacology; D013055:Spectrophotometry, Infrared
D002316:Cardiotonic Agents; D011720:Pyrazoles; D011728:Pyridones