Synthesis of a New Series of Heterocyclic Scaffolds for Medicinal Purposes

Hikmat S. Hilal's picture
Journal Title, Volume, Page: 
European Journal of Medicinal Chemistry Volume 41, Issue 8, August 2006, Pages 1017-1024
Year of Publication: 
2006
Authors: 
H.S. Hilal
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
Current Affiliation: 
Department of Chemistry, An-Najah N. University, Nablus, PO Box 7, West Bank, Palestine
M.S. Ali-Shtayeh
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
R. Arafat
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
T. Al-Tel
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
W. Voelter
Abteilung für Physikalische Biochemie des Physiologisch-Chemischen Instituts der Universität Tübingen, Hoppe-Seyler Straße 4, 72076 Tübingen, Germany
A. Barakat
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
Preferred Abstract (Original): 

A new series of substituted 8-fluro-4H-pyrimido[2,1-b] [1,3]benzothiazole-4-ones () substituted 7-methyl-4H-isoxazolo[2,3-a]pyrimidin-4-ones, and substituted 2-methyl-5,6,7,8-tetrahydro-9H-isoxazolo[2,3-a]pyridopyrimidin-9-ones, compounds I–VII, have been prepared via condensation of β-keto esters with 2-aminopyridine derivatives, in the presence of polyphosphoric acid. The same technique has also been used to prepare diazepine compounds, VIII–X, by condensation of a γ-keto ester with 2-aminopyridine derivatives. Details of synthetic procedures are shown. The new compounds have been characterized by elemental analysis, GC–MS, FT-IR and NMR spectrometry. Antibacterial, antifungal and anticancer (cytotoxic) activities, for three of these compounds, have been investigated and are presented.

Synthesis of a new series of heterocyclic scaffolds for medicinal purposes

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