Hilal H S, Ali-Shtayeh M S, Arafat R, Al-Tel T, Voelter W, Barakat A
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine.
Eur J Med Chem. 2006 Aug;41(8):1017-24. doi: 10.1016/j.ejmech.2006.03.025. Epub 2006 Jun 22.
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 beta-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 gamma-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.
通过β-酮酯与2-氨基吡啶衍生物在多磷酸存在下缩合，制备了一系列新的取代的8-氟-4H-嘧啶并[2,1-b][1,3]苯并噻唑-4-酮（）、取代的7-甲基-4H-异恶唑并[2,3-a]嘧啶-4-酮以及取代的2-甲基-5,6,7,8-四氢-9H-异恶唑并[2,3-a]吡啶并嘧啶-9-酮，即化合物I-VII。相同的技术也被用于通过γ-酮酯与2-氨基吡啶衍生物缩合制备二氮杂卓化合物VIII-X。展示了合成步骤的细节。这些新化合物已通过元素分析、气相色谱-质谱联用、傅里叶变换红外光谱和核磁共振光谱进行了表征。对其中三种化合物的抗菌、抗真菌和抗癌（细胞毒性）活性进行了研究并予以呈现。
