SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS | ||||
Bulletin of Pharmaceutical Sciences Assiut University | ||||
Article 1, Volume 34, Issue 2, 2011, Page 159-179 PDF (769.33 K) | ||||
Document Type: Original Article | ||||
DOI: 10.21608/bfsa.2011.63272 | ||||
View on SCiNiTO | ||||
Authors | ||||
Salah A. Abdel-Aziz1; Nawal A. El-Koussi2; Hoda Y. Hassan2; Adel F. Youssef2; Magda M. Yousri3 | ||||
1Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Al-Azhar University | ||||
2Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University | ||||
3Department of Pharmacology, Faculty of Medicine, Assiut University | ||||
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. | ||||
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