SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS

Abdel-Aziz, Salah A.; El-Koussi, Nawal A.; Hassan, Hoda Y.; Youssef, Adel F.; Yousri, Magda M.

doi:10.21608/bfsa.2011.63272

SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS

Document Type : Original Article

Authors

¹ Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Al-Azhar University

² Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University

³ Department of Pharmacology, Faculty of Medicine, Assiut University

10.21608/bfsa.2011.63272

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.