Rose U
Institut für Pharmazie, Johannes Gutenberg-Universität Mainz.
Arch Pharm (Weinheim). 1990 May;323(5):281-6. doi: 10.1002/ardp.19903230506.
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.
通过环己二酮(1)与芳香醛2a - I的Knoevenagel反应以及随后与β-氨基巴豆酸甲酯3进行环化迈克尔加成反应制备了六氢喹啉酮4a - I。这些新化合物通过红外光谱、¹H - NMR光谱和质谱进行表征。在电刺激的豚鼠左心房中,4型结构显示出明显的正性肌力作用,而BaCl₂诱导的豚鼠回肠收缩则呈剂量依赖性受到抑制,其活性与硝苯地平相当。此外,还观察到氯化钾刺激的主动脉平滑肌的舒张。