N-Hydroxyamide, alkanoloamides, dialkylamino-alkylamides and some of morpholinealkylamides of pyrimidin-8-on[2,1-f]theophylline-9-alkylcarboxylic acids were prepared and preliminary tested for their cardiovascular activity. Some of the tested compounds presented effects on arrhythmia parameters and blood pressure. The most interesting were dialkylamino-alkylamides and their morpholine analogs (4a-10a), which protected the heart against the bradycardia and diminished mortality of animals. In comparison to the chinidini sulfas the strongest activity was observed for diethylaminoethylamide of pyrimidin-8-on[2,1- f]theophylline-9-acetic acid (4a). Amides (1-3) without the basic center in the substituent showed weak antihypertensive properties.
Keywords: Antiarrhythmic agents, adenosine receptors antagonists, pyrimido[2,1-f-]theophylline-9-alkylcarboxylic acids amides, cardiovascular activity of fused [2,1-f]theophyllines, tricyclic theophylline derivatives
Rights & PermissionsPrintExport