[Hexahydroquinolinones with calcium-modulatory effects--synthesis and pharmacologic action].
The hexahydroquinolinones 4a-I were prepared by Knoevenagel-reaction of cyclohexandione (1) and the aromatic aldehydes 2a-I and subsequent cyclising Michael-addition with methyl beta-aminocrotonate 3. The new compounds are characterized by IR-, 1H-NMR-and mass spectroscopy. At the electrically stimulated left guinea pig-atrium structures of type 4 show marked positive inotropic effects, whereas BaCl2-induced contractions of the guinea pig-ileum are supressed dose-dependently with activity rates comparable to those of nifedipine. Furthermore, relaxation of KCl-stimulated aorta-musculature is observed.
Rose
U
U
Institut für Pharmazie, Johannes Gutenberg-Universität Mainz.
D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D013055:Spectrophotometry, Infrared
D002121:Calcium Channel Blockers; D015363:Quinolones
Hexahydrochinolinone mit calciummodulatorischem Effekt--Synthese und pharmakologische Wirkung.