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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


    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


    Abteilung für Physikalische Biochemie des Physiologisch-Chemischen Instituts der Universität Tübingen, Hoppe-Seyler Straße 4, 72076 Tübingen, Germany


    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 IVII, have been prepared via condensation


    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.

    © 2006 Elsevier SAS. All rights reserved.

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Hikmat S. Hilal
Organometallics (organic and inorganic), Materials, Catalysis, Semiconductors, Photoelectro-chemistry
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