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- Thursday, March 16, 2006
- Synthesis of a new series of heterocyclic scaffolds for medicinal purposes
- Published at:Not Found
European Journal of Medicinal Chemistry 41 (2006) 1017
–1024.
H.S. Hilal
a,*, M.S. Ali-Shtayeh a, R. Arafat a, T. Al-Tel a, W. Voelter b, A. Barakat
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
b
Abteilung für Physikalische Biochemie des Physiologisch-Chemischen Instituts der Universität Tübingen, Hoppe-Seyler Straße 4, 72076 Tübingen, Germany
Abstract
A new series of substituted 8-fluro-4
H-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-9
H-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.
© 2006 Elsevier SAS. All rights reserved.
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