An-Najah Staff

A new series of substituted 8-fluoro-4H-pyrimido[2, l-b][l,3] benzo- thiazole-4-ones (24) and (25), substituted 7-methyl-4H-isoxazolo[2, 3-a] pyrimidin-4-ones (26-28), and substituted 2-methyl-5,6,7,8-tetrahydro-9H- isoxazolo[2, 3-a] pyridopyrimidin-9-ones (29) and (30), have been prepared via condensation of β- keto esters with 2-aminopyridine derivatives. Furthermore diazipine Compounds (31-33) have been prepared via condensation of a γ-keto ester with 2-aminopyridine derivatives. The reactions were conducted in the presence of poly phosphoric acid (PPA). The details of the synthesis procedures are described. The new compounds have been characterized using elemental analysis, GC MS, FT IR and NMR spectrometry. Compounds 24, 27 and 28 were tested against Staphylococcus aureus, proteus vulgaris, and candida albicans bacteria. None of the three compounds showed antibacterial activity. The same compounds were tested against Microsporum canis, jusiarium tricincutum, pythium ultimum, pythium aphanidermatum, and pythium midlletonii fungi types. All of them showed antifungal activity. Compounds 27, 32 and 33 were tested for anticancer activity by the MTT assay. They all showed significant anticancer activity.