Studies on Calcium Antagonist Activities of 2-Ethyl-3-carbmethoxy-4-aryl-5-oxo-6,6-dimethyl-1,4,5,6,7,8-hexahydroquinoline Derivatives

 

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Summary

In this study, 23 new compounds having 2-ethyl-3-carbmethoxy-4-aryl-5-oxo-6,6-dimethyl-1,4,5,6,7,8-hexahydroquinoline structure have been synthesised and screened for their calcium antagonistic activities. The structure of the compounds were characterised by IR, ¹H-NMR, ¹³C-NMR, mass spectroscopy and elemental analyses. The calcium antagonistic activities of the compounds were determined by the tests performed on isolated rat ileum and lamb carotid artery. Although none of the synthesized compounds were as active as nicardipine in isolated rat ileum, the compounds 9, 10 and 19 have shown high activity. In screening studies on lamb carotid artery, compounds 10, 14 and 19 have been found active at a concentration of 10⁻⁴ mol/l.

Zusammenfassung

Studien zur Kalzium-antagonistischen Wirkung von 2-Ethyl-3-carbmethoxy-4-aryl-5-oxo-6,6-dimethyl-1,4,5,6,7,8-hexa hydrochinolin-Derivaten

Es wurden 23 neue 2-Ethyl-3-carbme thoxy-4-aryl-5-oxo-6,6-dimethyl-1,4,5,6,7,8-hexahydrochinolin-Derivate (Verbindungen 1–23) synthetisiert. Die Strukturaufklärung erfolgte IR-, ¹H-NMR-, ¹³C-NMR- und massenspektrome-trisch sowie mittels Elementaranalyse. Die Kalzium-antagonistischen Eigenschaften der Verbindungen wurden am isolierten Kaninchenileum und der Lammkarotis untersucht. Die Verbindungen 9, 10 und 19 zeigten in den Tests am isolierten Kaninchenileum die höchste Aktivität, die Verbindungen 10, 14 und 19 waren in den Lammkarotis-Tests am aktivsten.