[Synthesis and cardiotonic activity of pyrazolylpyrimidines].
A series of pyrazolylpyrimidines was prepared by the reaction of hydrazinopyrimidines and pyrimidinecarbohydrazides with acetylacetone, and was screened for cardiotonic activity in papillary muscles and atrium of guinea-pig hearts. Many of these compounds were found to be active, and 2-(4,5-dimethyl-pyrazol-1-yl)-4-thioxo-6-methyl-4 H-pyrimidine (1c), 2-methylthio-pyrimidine-4-yl-hydroxyacet-(5-hydroxy-3,5-dimethyl)- 1-5 H-pyrazolide (7a) and 2-methylthio-4-oxo-4 H-pyrimidine-3-yl-acet-(5-hydroxy-3,5-dimethyl)-1-5 H-pyrazolide (7b) showed the most positive-inotropic effects. The ED50 values are close to those of milrinone.
Sedereviciute
V
V
Chemische Fakultät der Universität Vilnius, Germany.
Garaliene
V
V
Vainilavicius
P
P
Hetzheim
A
A
D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004558:Electric Stimulation; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009200:Myocardial Contraction / Q000187:drug effects; D010210:Papillary Muscles / Q000187:drug effects; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology
D002316:Cardiotonic Agents; D011743:Pyrimidines
Synthese und kardiotone Aktivität von Pyrazolylpyrimidinen.