Author/Authors :
Abdel-Aziz, Salah A. Al-Azhar University - Faculty of Pharmacy - Department of Pharmaceutical Medicinal Chemistry, Egypt , El-Koussi, Nawal A. Assiut University - Faculty of Pharmacy - Department of Medicinal Chemistry, Egypt , Hassan, Hoda Y. Assiut University - Faculty of Pharmacy - Department of Medicinal Chemistry, Egypt , Youssef, Adel F. Assiut University - Faculty of Pharmacy - Department of Medicinal Chemistry, Egypt , Yousri, Magda M. Assiut University - Faculty of Medicine - Department of Pharmacology, Egypt
Abstract :
A series of Dihydropyrimidines (DHPMs) with variable substituents at four positions in pyrimidine nucleus (I-IV), were prepared and tested for their calcium channel blocker and hypotensive effect using amlodipine as a reference compound. Molecular alignment revealed a direct correlation between fitting and in-vitro rat ileum relaxation. A pharmacophore was developed for compounds with hypotensive and/or calcium channel blocking activity. Series IV showed hypotensive and calcium antagonist effect, while series I and II showed calcium antagonist activity without hypotensive action. Series III were devoid of either effect.
