Simsek, Rahime; Safak, Cihat; Erol, Kevser; Ataman, Sule; Ulgen, Mert; Linden, Anthony published the artcile< Synthesis, evaluation of the calcium antagonistic activity and biotransformation of hexahydroquinoline and furoquinoline derivatives>, Application In Synthesis of 112-63-0, the main research area is calcium antagonist hexahydroquinoline furoquinoline structure activity.
The objective of this study was to synthesize 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-hexahydroquinoline derivatives were synthesized by modified Hantzsch synthesis and 1,3,4,5,6,7,8,9-octahydro-7,7-dimethyl-9-arylfuro[3,4-b]quinoline-1,8-dione derivatives were synthesized 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. Some of these compounds showed high tissue selectivity compared with nicardipine. In the hexahydroquinoline series, the compounds having ortho substituted Ph substituent were more active than the meta isomers. Lactone derivatives were found less active than hexahydroquinoline derivatives in respect to calcium antagonistic activity.
Arzneimittel-Forschung published new progress about Calcium channel blockers. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application In Synthesis of 112-63-0.
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