Studies on the synthesis and biological activitiy of 6-ethyl-4-aryl-5-methoxycarbonyl-3,4-dihydropyrimidin-2(1H)-ones

Sarac S., Ciftci M., Zorkun İ. S., Tunc O., Erol K.

ARZNEIMITTELFORSCHUNG-DRUG RESEARCH, cilt.57, sa.3, ss.137-142, 2007 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 57 Sayı: 3
  • Basım Tarihi: 2007
  • Doi Numarası: 10.1055/s-0031-1296596
  • Dergi Adı: ARZNEIMITTELFORSCHUNG-DRUG RESEARCH
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.137-142
  • Karadeniz Teknik Üniversitesi Adresli: Hayır

Özet

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.