[New biologically active theophylline derivatives. Synthesis and pharmacologic properties of flufylline and fluprofylline].
Within the course of the research project for finding new cardiovascular drugs we have synthetized since 1976 piperazine- and piperidine derivatives of theophylline. The screening shows for the substances Sgd 19578 (flufylline) and Sgd 14480 (fluprofylline) a long-lasting blood pressure lowering activity as well as a remarkable serotonin- and histamine antagonism and broncholytic activity. On the basis of these results these compounds were selected for further investigation.
D006916:5-Hydroxytryptophan / Q000037:antagonists & inhibitors; D000818:Animals; D000893:Anti-Inflammatory Agents; D001794:Blood Pressure / Q000187:drug effects; D001980:Bronchi / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006633:Histamine Antagonists; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D051381:Rats; D013806:Theophylline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D014590:Uterine Contraction / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D006633:Histamine Antagonists; C040397:fluprophylline; D013806:Theophylline; D006916:5-Hydroxytryptophan; C040398:flufylline
Neue biologisch aktive Theophyllin-Derivate. Synthese und pharmakologische Eigenschaften von Flufyllin und Fluprofyllin.