Arzneimittelforschung 2006; 56(7): 529-534
DOI: 10.1055/s-0031-1296747
Antihypertensives
Editio Cantor Verlag Aulendorf (Germany)

4-Difluoro-substituted Phenyl-5-oxo-hexahydroquinoline Derivatives and Their Effects on Calcium Channels

Rahime Şimşek
1   Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey
,
Miyase Gözde Gündüz
1   Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey
,
Başar Sirmagül
2   Department of Pharmacology, Faculty of Medicine, Osman Gazi University, Eskişehir, Turkey
,
Cihat Şafak
1   Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey
,
Kevser Erol
2   Department of Pharmacology, Faculty of Medicine, Osman Gazi University, Eskişehir, Turkey
,
Anthony Linden
3   Institute of Organic Chemistry, University of Zurich, Switzerland
› Institutsangaben
Weitere Informationen

Publikationsverlauf

Publikationsdatum:
22. Dezember 2011 (online)

Summary

Twenty new methyl(ethyl) 2,6,6- or 2,7,7-trimethyl-5-oxo-4-(disubstituted phenyl)-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates and ten new N,N-diethyl-2,6,6- or 2,7,7-trimethyl-5-oxo-4-(disubstituted phenyl)-l,4,5,6,7,8-hexahydroquinoline-3-carboxamide derivatives have been synthesised and screened for their calcium channel antagonistic activity. The compounds were synthesised by the Hantzsch reaction. Calcium antagonistic activities of the compounds were determined by the tests performed on isolated rat ileum and rat thoracic artery.

Zusammenfassung

4-Difluor-substituierte Phenyl-5-oxohexahydrochinolin-Derivate und ihre Wirkungen auf Kalziumkanäle

Zwanzig neue Methyl(ethyl)-2.6.6-oder -2,7,7-trimethyl-5-oxo-4-(disubstituierte Phenyl)-l,4,5,6,7,8-hexahydrochinolin-3-carboxylate und 10 neue N,N-Diethyl-2,6,6- oder -2,7,7-trimethyl-5-oxo-4-(disubstituierte Phenyl)-l,4,5,6,7,8-hexahydrochinolin-3-carboxamid-Derivate wurden synthetisiert und auf ihre Kalziumkanal-antagonistische Wirkung untersucht. Die Synthese erfolgte durch Hantzsch-Reaktion. Die Kalziumantagonistischen Wirkungen der Substanzen wurden durch Tests an isolierten Arterien aus Ileum und Thorax von Ratten untersucht.