Studies on the synthesis and biological activitiy of 6-ethyl-4-aryl-5-methoxycarbonyl-3,4-dihydropyrimidin-2(1H)-ones
| Autor: | Selma Saraç, Ozgül Tunc, Inci Selin Zorkun, Murat Ciftci, Kevser Erol |
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| Rok vydání: | 2007 |
| Předmět: |
Male
Magnetic Resonance Spectroscopy Stereochemistry Biginelli reaction Nicardipine Pyrimidinones In Vitro Techniques Muscle Smooth Vascular Catalysis chemistry.chemical_compound Ileum Drug Discovery medicine Animals Urea Aldehydes Ethanol Sheep Chemistry Aryl Biological activity Muscle Smooth Nuclear magnetic resonance spectroscopy Calcium Channel Blockers Rats Carotid Arteries Benzaldehydes Female Indicators and Reagents Crystallization Nuclear chemistry medicine.drug Muscle Contraction |
| Zdroj: | Arzneimittel-Forschung. 57(3) |
| ISSN: | 0004-4172 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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