Synthesis of a New Series of Heterocyclic Scaffolds for Medicinal Purposes

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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
Faculty of Science, An-Najah National University, Nablus. Palestine
M.S. Ali-Shtayeh
Faculty of Science, An-Najah National University, Nablus. Palestine
Current Affiliation: 
Department of Biology and Biotechnology, Faculty of Science, An-Najah National University, Nablus. Palestine
R. Arafat
Faculty of Science, An-Najah National University, Nablus. Palestine
T. Al-Tel
Faculty of Science, An-Najah National University, Nablus. Palestine
W. Voelter
Abteilung für Physikalische Biochemie des Physiologisch-Chemischen Instituts der Universität Tübingen, Hoppe-Seyler Straße 4, 72076 Tübingen, Germany
A. Barakat
Faculty of Science, An-Najah National University, 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, VIIIX, 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.

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