Saraç Selma, Ciftçi Murat, Zorkun Inci Selin, Tunç Ozgül, Erol Kevser
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe Universitya, Ankara, Turkey.
Arzneimittelforschung. 2007;57(3):137-42. doi: 10.1055/s-0031-1296596.
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.
根据Biginelli反应，以HCl为催化剂，通过将尿素与3-氧代戊酸甲酯和芳香醛在无水乙醇中缩合，合成了6-乙基-4-芳基-5-甲氧基羰基-3,4-二氢嘧啶-2(1H)-酮衍生物(1-10)。通过光谱和元素分析确定了化合物的结构。通过对离体大鼠回肠和羔羊颈动脉进行的试验测定了化合物的钙通道阻滞活性。在离体大鼠回肠上，发现化合物2在10(-5)mol/L浓度下比尼卡地平（CAS 55985-32-5）更有效。在羔羊颈动脉上，化合物5、6以及化合物4、5、6分别在10(-6)mol/L和10(-5)mol/L浓度下具有显著活性。
