Studies on the synthesis and biological activitiy of 6-ethyl-4-aryl-5-methoxycarbonyl-3,4-dihydropyrimidin-2(1H)-ones.
6-Ethyl-4-aryl-5-methoxycarbonyl-3,4-dihydropyrimidin-2(1H)-one derivatives (1-10) were synthesized by condensing urea with methyl 3-oxopentanoate and aromatic aldehydes in absol. ethanol using HCl as a catalyst according to the Biginelli reaction. The structures of the compounds were confirmed by spectroscopic and elemental analysis. The calcium channel blocker activities of the compounds were determined by the tests performed on isolated rat ileum and lamb carotid artery. On the isolated rat ileum, compound 2 was found to be more effective at 10(-5) mol/L concentration than nicardipine (CAS 55985-32-5). On the lamb carotid artery compounds 5, 6 and 4, 5, 6 were significantly active at 10(-6) mol/L and 10(-5) mol/L concentrations, respectively.
Saraç
Selma
S
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe Universitya, Ankara, Turkey. sesarac@hacettepe.edu.tr
Ciftçi
Murat
M
Zorkun
Inci Selin
IS
Tunç
Ozgül
O
Erol
Kevser
K
D000447:Aldehydes; D000818:Animals; D001547:Benzaldehydes / Q000737:chemistry; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D002339:Carotid Arteries / Q000187:drug effects; D003460:Crystallization; D005260:Female; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D012756:Sheep; D014508:Urea / Q000737:chemistry
D000447:Aldehydes; D001547:Benzaldehydes; D002121:Calcium Channel Blockers; D007202:Indicators and Reagents; D011744:Pyrimidinones; D014508:Urea; C032175:benzaldehyde