SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS
Abdel-Aziz, S., El-Koussi, N., Hassan, H., Youssef, A., Yousri, M. (2011). SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS. EKB Journal Management System, 34(2), 159-179. doi: 10.21608/bfsa.2011.63272
Salah A. Abdel-Aziz; Nawal A. El-Koussi; Hoda Y. Hassan; Adel F. Youssef; Magda M. Yousri. "SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS". EKB Journal Management System, 34, 2, 2011, 159-179. doi: 10.21608/bfsa.2011.63272
Abdel-Aziz, S., El-Koussi, N., Hassan, H., Youssef, A., Yousri, M. (2011). 'SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS', EKB Journal Management System, 34(2), pp. 159-179. doi: 10.21608/bfsa.2011.63272
Abdel-Aziz, S., El-Koussi, N., Hassan, H., Youssef, A., Yousri, M. SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS. EKB Journal Management System, 2011; 34(2): 159-179. doi: 10.21608/bfsa.2011.63272

SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS

Bulletin of Pharmaceutical Sciences Assiut University
Article 1, Volume 34, Issue 2, 2011, Pages 159-179    PDF (769.33 K)
Document Type: Original Article
DOI: 10.21608/bfsa.2011.63272
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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