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.
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.
Simşek
R
R
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey. RahimeSimsek@hotmail.com
Safak
C
C
Erol
K
K
Sirmagül
B
B
D000818:Animals; D017609:Barium Compounds / Q000494:pharmacology; D002121:Calcium Channel Blockers / Q000737:chemistry / Q000494:pharmacology*; D002339:Carotid Arteries / Q000187:drug effects; D002712:Chlorides / Q000494:pharmacology; D002855:Chromatography, Thin Layer; D005260:Female; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009529:Nicardipine / Q000494:pharmacology; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D012756:Sheep; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D017609:Barium Compounds; D002121:Calcium Channel Blockers; D002712:Chlorides; D015363:Quinolones; C024986:barium chloride; D009529:Nicardipine