Synthesis, evaluation of the calcium antagonistic activity and biotransformation of hexahydroquinoline and furoquinoline derivatives

Simsek R. , Safak C. , Erol K., Ataman S., Ulgen M., Linden A.

ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH, cilt.53, sa.3, ss.159-166, 2003 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 53 Konu: 3
  • Basım Tarihi: 2003
  • Sayfa Sayıları: ss.159-166


The objective of this study was to synthesise new condensed 1,4-dihydropyridine derivatives and investigate their calcium channel blocking activity. In addition, the in vitro hepatic microsomal biotransformation of one hexahydroquinoline derivative was studied. 2,6,6-Trimethyl-3-carbmethoxy (carbethoxy)-4-aryl-5-oxo-1,4,5,6,7,8-hexahydroquinotine derivatives were synthesised by modified Hantzsch synthesis. I,3,4,5,6,7,8,9-octahydro-7,7-dimethyl-9-arylfuro [3,4-b]quinotine-1,8-dione derivatives were synthesised the reaction of hexahydroquinoline derivatives with pyridinium bromide perbromide. The calcium antagonistic activities of the compounds were determined by tests performed on isolated rat ileum and lamb carotid artery. In vitro hepatic biotransformation of one compound was studied in rat microsomes.